The nursing intervention of ultrasound drug penetration in the application of the digestive tract cancer patients′ postoperative rapid recovery / 中国实用护理杂志

Objective:To explore the impact of nursing intervention in strengthening the implementation of ultrasound drug penetration therapy on postoperative rapid recovery of patients with digestive tract tumors after surgery, and to provide reference for the formulation of intervention plans for postoperative rapid recovery of digestive tract tumor patients.Methods:A randomized controlled trial was used. From April to July 2021, 120 postoperative patients with digestive tract tumors admitted to the Second Affiliated Hospital of Dalian Medical University were selected and divided into a control group, a dispersed treatment group, and a concentrated treatment group according to the random number table method, with 40 patients in each group. The control group mainly received routine accelerated rehabilitation surgical care, supplemented by early rehabilitation training; the dispersed treatment group received nursing intervention with ultrasound drug penetration therapy on the basis of the control group, once a day in the morning and once in the afternoon, lasting for 30 min each time; on the basis of the control group, the concentrated treatment group received nursing intervention of one-time concentrated ultrasound drug penetration therapy for 60 min. The gastrointestinal reactions, intestinal function recovery, hospitalization, postoperative complications, and nursing satisfaction of each group of patients were observed and compared using one-way ANOVA, LSD- t test, and χ2 test. Results:There were 27 males and 13 females in the control group, aged (61.85 ± 16.85) years old. while 23 males and 17 females in the dispersed treatment group aged (60.90 ± 16.88) years old, and 23 males and 17 females in the concentrated treatment group aged (59.80 ± 13.58) years old. The duration of postoperative nausea, vomiting, and abdominal distension symptoms, recovery time of bowel sounds, recovery time of exhaust, and first meal time in the dispersed treatment group and concentrated treatment group were (38.58 ± 2.74), (17.45 ± 1.92), (38.76 ± 3.34), (50.04 ± 2.57) h and (36.79 ± 2.58), (16.48 ± 1.85), (36.98 ± 2.28), (48.25 ± 3.07) h, respectively, which were lower than those in the control group (43.13 ± 3.56), (21.24 ± 2.50) (42.65 ± 3.78), (52.21 ± 3.15) h, the differences were statistically significant ( t values were 3.38-9.68, all P<0.05). The duration of postoperative nausea, vomiting, and abdominal distension symptoms, recovery time of bowel sounds, recovery time of exhaust, and first meal time in the concentrated treatment group were shorter than those in the dispersed treatment group, and the differences were statistically significant ( t values were 2.31-3.01, all P<0.05). The time to get out of bed activity and hospitalization of patients in the dispersed treatment group and the concentrated treatment group were (5.83 ± 1.20) h, (9.90 ± 2.12) d and (7.35 ± 2.13) h, (8.30 ± 1.42) d, respectively. The control group was (4.39 ± 1.53) h and (14.93 ± 2.56) d, respectively. The time to get out of bed activity and hospitalization of patients in the dispersed treatment group and the concentrated treatment group were better than those in the control group, while the time to get out of bed activity and hospitalization of patients in the concentrated treatment group were better than those in the dispersed treatment group, the differences were statistically significant ( t values were -7.14-14.34, all P<0.05). The incidence of intestinal obstruction was 15.0% (6/40) in the control group, 5.0% (2/40) in the dispersed treatment group, and 0 in the concentrated treatment group, with a statistically significant difference ( χ2=7.50, P<0.05). The nursing satisfaction of patients in the concentrated treatment group reached 100.00% (40/40), which was 92.5% (37/40) and 85.0% (34/40) in the dispersed treatment group and control group, with a statistically significant difference ( χ2=6.49, P<0.05). Conclusions:Nursing intervention through ultrasound drug penetration therapy, especially centralized treatment, can significantly improve postoperative intestinal function, reduce postoperative gastrointestinal reactions, shorten hospitalization time, reduce postoperative complications, accelerate patient recovery, and provide effective nursing intervention plans for clinical practice. It is worth promoting and applying.

Effect of Terpenes on the enhancement of skin permeation of lipophilic drugs: A systematic review

Objectives@#The stratum corneum (SC) remains an obstacle to the passage of drugs applied topically. Several investigations have focused on enhancing the penetration of drugs through the SC by integrating permeation enhancers (PE) into the drug formulation. Terpenes are among the PE utilized in formulations and are categorized by the regulatory bodies as generally recognized as safe (GRAS). This study aimed to comparatively analyze the skin permeation enhancing effect of terpenes on lipophilic drugs. @*Methods@#The present study reviewed the effects of terpenes on the permeation of lipophilic small-molecule drugs through the skin using original research published between 2000 - 2022 retrieved from PubMed®. The search phrase used was (lipophilic drug) AND (terpene) AND (permeation enhancer). @*Results@#Terpenes increase the percutaneous permeation of lipophilic small molecule drugs by 1.06 – 256.80-fold. Linear correlation analysis of terpenes’ cLog P with enhancement ratio (ER) revealed moderate and strong positive correlations in pig skin (r = 0.21) and mouse skin (r = 0.27), and rat skin (r = 0.41) and human skin (r = 0.67), respectively. Drug cLog P is a poor (r = -0.06) predictor of permeation enhancement. Terpenes with cLog P higher than 2.40 had ER greater than 10. Higher ERs (>30) were recorded for nerolidol, carvacrol, borneol, terpineol, limonene, menthone, pulegone, and menthol among the terpene-chemical penetration enhancers. @*Conclusion@#cLog P of terpene-based chemical permeation enhancers (CPE) is strongly correlated with ER of lipophilic drugs across human skin. Non-polar groups in terpenes and hydrogen bond interactions by terpenes with SC lipid enhance cutaneous drug penetration of lipophilic drugs.

MICRONEEDLES ASSISTED ENHANCEMENT OF TRANSDERMAL DELIVERY OF CURCUMIN THROUGH ORGANOGEL FORMULATION

Curcumin is a natural compound found in turmeric and has been shown to have anti-inflammatory and antioxidant properties. Topical delivery of curcumin through an organic emulsion-based gel can effectively target inflammation at specific sites on the body. The current study aims to formulate Pluronic based organogel of curcumin, whose absorption is further assisted by microneedles technology. Nine organogel formulations were prepared and optimized by 32 full factorization model to fix the ratio of lecithin[A] and Pluronic[B] concentration in order to get optimum drug release after 2 hours (Q2) and maximum release of drug after 8 hours (Q8). The in-vitro study through the Franz diffusion cell indicated a significant impact of Pluronic F-127 concentration on the release of drug. As increased concentration of Pluronic increased the viscosity of formulations which ultimately retarded the release of drug. Based on Design of Experiment (DoE) study, optimized batch containing 6.5% lecithin and 20.6% Pluronic was further studied for microneedle assisted ex-vivo skin permeation through rat skin. Permeation without microneedle poration was around 70.26% after 8 hours, which was significantly increased (around 25%) after microneedle treatment of the skin. The results indicated promising application microneedle assisted skin permeation as a non-invasive and controlled delivery of curcumin through the transdermal route. Further, in-vivo studies are recommended to further establish this promising concept, targeting a variety of inflammatory conditions, including arthritis, psoriasis, and eczema, etc., through non-invasive transdermal drug delivery systems.

Tritium permeation resistance of Al-Al₂O₃ coatings prepared by thermal spraying / 中国辐射卫生

@#<b>Objective</b> To make the preparation method for coatings more convenient in the field where the requirements for tritium permeation resistance are not high, this paper proposes a method for preparing Al-Al₂O₃ tritium permeation barriers by thermal spraying technology and conducts a performance analysis. <b>Methods</b> The tritium permeation resistance and adhesion of Al-Al₂O₃ coatings prepared by thermal spraying were verified by experiments. <b>Results</b> The tritium permeability was reduced by one order of magnitude after a 0.2-mm Al-Al₂O₃ coating was sprayed on the stainless steel surface, and the tritium permeation resistance had no significant improvement with the increase in coating thickness; the adhesion of the coating was determined in the range of 5-10 N by scratch tests. <b>Conclusion</b> In this paper, a simple preparation method for tritium permeation barrier is proposed, and the tritium permeation resistance performance of Al-Al₂O₃ coatings prepared by thermal spraying technology is determined, which provides a reference for the selection of tritium permeation barrier in the field of tritium-containing solid waste storage.

Application progress of parallel artificial membrane permeation assay model in drug permeability screening of transdermal drug delivery system / 中国药房

The traditional model Franz diffusion cell method has always been the “gold standard” for evaluating the permeability of transdermal drug delivery system （TDDS） drug. However， in the high throughput screening of a large number of drug molecules， it has the disadvantages of low efficiency， high cost， difficulty to obtain isolated skin，poor reliability and large workload. The emergence of parallel artificial membrane permeation assay （PAMPA） model provides reliable pre-prediction data for the evaluation of permeability of TDDS drug. PAMPA model has been widely used in the permeability screening research of TDDS drugs and their preparations such as analgesics， local anesthetics， antioxidants， antipyretics， analgesics and anti-inflammatory drugs， vitamins， cholinesterase inhibitors， active ingredients of natural products， and has the characteristics of high reliability， good selectivity， high efficiency， low cost and data stability. PAMPA model has greatly improved the high throughput screening efficiency of TDDS drug permeability. With the extensive application and gradual maturity of this model， it will become a new and effective evaluation method in addition to the traditional evaluation model.

Advance of hair follicle targeted drug delivery systems in the treatment of acne and hair loss / 药学学报

Hair follicle (HF), one of the skin appendages, has received a lot of attention to be a new target and pathway for drug delivery. The development of hair follicle targeted drug delivery system (HFTDDS) through percutaneous permeation is particularly important for skin diseases derived from HF such as acne, hair loss, and folliculitis for their on-site action. This review describes the structure and physiological function of HF, the microenvironment of HF, and factors affecting HF permeation. Multiple nanoformulations used to improve the HF permeation and technologies to characterize the HF permeation were introduced. The latest advance of HFTDDS based on nanoformulations were systematically summarized and analyzed in the treatment of acne and hair loss. Finally, the challenges of formulating HFTDDS were discussed. The review is expected to provide some ideas and references for developing delivery systems for treating skin diseases derived from HF.

In-Vitro and Ex-Vivo Evaluation of Transfersomal Gel of Methotrexate

Abstract Methotrexate on its oral and intravenous administration results in unwanted adverse effects. This drawback can be overcome by transdermal delivery because of its painless objective for systemic drug administration. Transfersomes are ultra-deformable vesicles with the flexibility to reach deeper tissues of the skin. The objective of this research work was to develop methotrexate transfersomal gel by thin film hydration technique, evaluated for entrapment efficiency, deformability, mean vesicle size, and stability, and incorporated into carbopol gel for ease of handling and skin applicability for a longer period of retention on skin. MTX-TFS gel & conventional gel were characterized for consistency, transparency, viscosity, and pH. Ex-vivo skin permeation studies were performed using abdominal goat skin and drug release kinetic parameters and transdermal flux were calculated using mathematical models. The results indicate that MTX was successfully entrapped (84.77 ± 2.35 %w/w) in transfersomes having 240±1.6 nm vesicle sizes and 27.13±0.7 deformability index. The gel was permeated through the skin at a rate of 28.12±2.58 µg/cm2/hr as compared to the conventional gel (10.35±2.14 µg/cm2/ hr). From the study, it was concluded that the MTX-TFS gel can be used as a possible substitute for the conventional formulation for transdermal drug delivery due to 3 times improvement in transdermal flux.

Locust bean gum hydrogels are bioadhesive and improve indole-3-carbinol cutaneous permeation: influence of the polysaccharide concentration

Abstract The locust bean gum (LBG) is a polysaccharide with thickening, stabilizing and gelling properties and it has been used in the preparation of pharmaceutical formulations. Hydrogels (HGs) are obtained from natural or synthetic materials that present interesting properties for skin application. This study aimed to develop HGs from LBG using indole-3-carbinol (I3C) as an asset model for cutaneous application. HGs were prepared by dispersing LBG (2%, 3% and 4% w/v) directly in cold water. The formulations showed content close to 0.5 mg/g (HPLC) and pH ranging from 7.25 to 7.41 (potentiometry). The spreadability factor (parallel plate method) was inversely proportional to LBG concentration. The rheological evaluation (rotational viscometer) demonstrated a non-Newtonian pseudoplastic flow behavior (Ostwald De Weale model), which is interesting for cutaneous application. The HET-CAM evaluation showed the non-irritating characteristic of the formulations. The bioadhesive potential demonstrated bioadhesion in a concentration-dependent manner. Permeation in human skin using Franz cells showed that the highest LBG concentration improved the skin distribution profile with greater I3C amounts in the viable skin layers. The present study demonstrated the feasibility of preparing HGs with LBG and the formulation with the highest polymer concentration was the most promising to transport active ingredients through the skin.

Impact of ferulic acid and resveratrol on the effectiveness and safety of sunscreen

Abstract The combination of avobenzone (AVO) and octyl ρ-methoxycinnamate (OMC) is widely used to ensure broad-spectrum photo-protection because they absorb UVA and UVB, respectively. However, they are thermally and photo unstable because they degrade and undergo photo- tautomerization and trans-cis isomerization, thus reducing their photo-protection efficacy during UV exposure. This study aimed to evaluate the potential use of the antioxidants ferulic acid and resveratrol as stabilizing substances in AVO and OMC mixtures in solution or emulsion. The effects of both antioxidants on the thermal/photo-stability and suppression of the filter singlet state, besides skin permeation, were evaluated. Both antioxidants contributed to preserving OMC and AVO during the thermal stability test, which relates to the maintenance of photo-protection even after storing the formulations at high temperatures. Nevertheless, although resveratrol retained part of the OMC trans isomer and suppressed the AVO singlet state when exposed to UV, no contribution to photo-protection stability was observed, contrary to expectations. Regarding the permeation assay, the addition of both antioxidants was accompanied by a reduction of AVO permeation, while resveratrol increased OMC permeation. Thus, the chemical and physicochemical properties of these antioxidants impacted their efficacy and safety profiles; therefore, further studies are required to establish the real cost-benefit ratio for their use in sunscreens.

Development, physicochemical evaluation, and in vivo permeation studies of topical formulations containing 0.1% tacrolimus

Abstract The objective of this paper was to develop and evaluate two semi-solid pharmaceutical forms containing 0.1% tacrolimus: cream (CRT01) and gel (GLT01). For the evaluation of physicochemical stability, at times 0, 30, 60 and 90 days, at 23°C and at 40°C, High Performance Liquid Chromatography coupled with a Diode Array Detector (HPLC-DAD) was employed. This method was developed and validated for tacrolimus quantification. The occlusivity test and skin permeation assay were also performed, using an animal model (Wistar rats), and the CRT01 and GLT01 were compared to the 0.1% tacrolimus ointment (PFU01) obtained from the University Pharmacy, Federal University of Rio de Janeiro, Brazil. CRT01 and GLT01 presented a homogeneous aspect and consistency adequate for topical products, along with sensory characteristics above PFU01. They also presented adequate physicochemical stability for 90 days and a lower occlusive effect than PFU01 (p<0.05). CRT01 showed greater affinity for the skin when compared to PFU01 and GLT01, with low systemic absorption. The CRT01 semi-solid formulation was considered the most adequate one to treat patients with atopic dermatitis or other dermatologic inflammatory diseases, promoting rational use of tacrolimus

Analysis of docosanol using GC/MS:Method development,validation,and application to ex vivo human skin permeation studies / 药物分析学报

Docosanol is the only US Food and Drug Administration(FDA)approved over-the-counter topical product for treating recurrent oral-facial herpes simplex labialis.Validated analytical methods for docosanol are required to demonstrate the bioequivalence of docosanol topical products.A gas chromatography/selected ion monitoring mode mass spectrometry(GC/SIM-MS)method was developed and validated for docosanol determination in biological samples.Docosanol and isopropyl palmitate(internal standard)were separated on a high-polarity GC capillary column with(88％cyanopropy)aryl-polysiloxane employed as the stationary phase.The ions of m/z 83 and 256 were selected to monitor docosanol and isopropyl palmitate,respectively;the total run time was 20 min.The GC/SIM-MS method was validated in accordance with US FDA guidelines,and the results met the US FDA acceptance criteria.The docosanol calibration standards were linear in the 100-10000 ng/mL concentration range(R2＞0.994).The recoveries for docosanol from the receptor fluid and skin homogenates were＞93.2％and＞95.8％,respectively.The validated method was successfully applied to analyze ex vivo human cadaver skin permeation samples.On applying Abreva?cream tube and Abreva?cream pump,the amount of doco-sanol that penetrated human cadaver skin at 48 h was 21.5±7.01 and 24.0±6.95 ng/mg,respectively.Accordingly,we concluded that the validated GC/SIM-MS was sensitive,specific,and suitable for quantifying docosanol as a quality control tool.This method can be used for routine analysis as a cost-effective alternative to other techniques.

Advances in the study of peptide drugs in oral drug delivery system / 药学学报

Peptide drugs exhibit an irreplaceable role in clinics due to their high specificity, efficiency and low toxicity. At present, more than 80 peptide drugs have been approved for marketing with global sales exceeding $50 billion in 2019. However, with large molecular weights, high hydrophilicity and instability in digestive tract, oral peptide drugs encounter substantial physiological barriers leading to low oral bioavailability. Therefore, peptide drugs are mostly administered by parenteral routes. Although parenteral delivery of peptide drugs achieves high bioavailability, this is associated with inconvenience and discomfort, even causing severe side effects compared with the oral route possessing a high degree of patient compliance. Therefore, numerous studies concentrate on novel strategies to improve the oral bioavailability of peptide drugs. Some delivery technologies such as Eligen™ and Axcess™ have been successfully applied to the oral dosage form of therapeutic peptides and have accelerated relevant oral formulations for Food and Drug Administration (FDA) approval and clinical treatment. In this review, we focus on the oral peptide delivery, mainly summarizing the progress of recent strategies used to overcome oral barriers and the commercialization applications of related patents, which could facilitate the research and development (R&D) of clinical applications of oral delivery techniques for peptide drugs.

Challenges of nanotechnology in cosmetic permeation with caffeine / Desafios da nanotecnologia na permeação cosmética com cafeína

The evolution of beauty market and personal care is constant in Brazil as well in the rest of the world. Technological advances have brought up nanotechnology to the cosmetological field, employing active principles at atoms enveloped by vesicles, in order to take the active principle precisely to the target tissue to optimize the results achieved because of the considerable ease to cross skin barriers. Manufacturing of nanotechnology cosmetics is confronted with low absorption capacity. One of the many active principle found in cosmetic industry is caffeine, a pseudoalkaloid from the xanthine group used as a stimulant with the mechanism of the lipolytic action. This active is widely used in a esthetics and cosmetics field in treatments involving dysfunctions such as localized fat and fibroedema geloid. To work out perfectly, the principle active need to interact and create a set of factors that includes lipolysis intensification. The caffeine encapsulation in gel-based nanocosmetics has the purpose of taking this active up to the adipocyte, the target cell, for mentioned dysfunctions treatment. Thus, we aim to present a review of how has been, the use of caffeine in the production of cosmetics.

A evolução do mercado de beleza e cuidados pessoais é constante no Brasil e no resto do mundo. Os avanços tecnológicos trouxeram a nanotecnologia para o campo cosmetológico, empregando princípios ativos em átomos envolvidos por vesículas, a fim de levar o princípio ativo precisamente ao tecido alvo para otimizar os resultados alcançados devido à considerável facilidade de atravessar barreiras cutâneas. A fabricação de cosméticos nanotecnológicos é confrontada com baixa capacidade de absorção. Um dos muitos princípios ativos encontrados na indústria cosmética é a cafeína, um pseudoalocalóide do grupo xantina usado como estimulante no mecanismo da ação lipolítica. Este ativo é amplamente utilizado no campo da estética e dos cosméticos em tratamentos que envolvem disfunções, como gordura localizada e fibroedema gelóide. Para funcionar perfeitamente, o princípio ativo precisa interagir e criar um conjunto de fatores que inclui a intensificação da lipólise. O encapsulamento de cafeína em nanocosméticos à base de gel tem o objetivo de levar esse ativo até o adipócito, a célula alvo, para o tratamento de disfunções mencionado. Assim, objetivamos apresentar uma revisão de como tem sido o uso de cafeína na produção de cosméticos.

Quality of cosmetics with active caffeine in cream and gel galenic bases prepared by compounding pharmacies / Qualidade de cosméticos com cafeína ativa em bases galênicas em creme e gel preparadas por farmácias de manipulação

As there is a great scarcity of studies on the importance of good compounding practices in the preparation of cosmetics, this study aimed to evaluate the quality control of cosmetics with active ingredient caffeine for the treatment of cellulite prepared by magistrals pharmacies. Microbiological analyzes, pH determination, color measurement, quantification of the percentage of the active ingredient caffeine and viscosity in creams and gels with 5% of the active ingredient caffeine were performed. In the microbiological analysis, the presence of molds and yeasts was verified above the permitted level according to the Brazilian pharmacopoeia. The pH decreased over time, contributing to the formulations becoming more acidic. In the color parameters, it was found that pharmacy F4 showed a brownish color, both for the gel and for the cream. The percentage of caffeine was within specifications in all formulations and the viscosity remained unchanged during the shelf life of the samples. It is important that the compounding pharmacies demand more effectively the commitment of the team, as well as the analysis of the raw material according to the microbiological control regulations to translate into the quality of the products prepared by the pharmacies and favor the consumer in the effective objective that the product you want to achieve.

Como há uma grande escassez de estudos sobre a importância de boas práticas de manipulação na elaboração de cosméticos, o presente estudo teve como objetivo avaliar o controle de qualidade de cosméticos com princípio ativo cafeína para o tratamento de celulite, elaborados por farmácias de manipulação de Campo Mourão. Foram realizadas análises microbiológicas, determinação do pH, mensuração da coloração, quantificação da porcentagem do princípio ativo cafeína e viscosidade em cremes e geís com 5% do princípio ativo cafeína. Nas análises microbiológicas foi verificada a presença de bolores e leveduras acima do pemitido segundo a farmacopéia brasileira. O pH diminuiu ao longo do tempo, contribuindo para que as formulações ficassem mais ácidas. Nos parâmetros de cor averiguou-se que a farmácia F4 apresentou uma coloração amarronzada, tanto para o gel quanto para o creme. A porcentagem de cafeína estava dentro das especificações em todas as formulações e a viscosidade se manteve inalterada durante o prazo de validade das amostras. Com o propósito de um melhor preparo magistral é importante que as farmácias de manipulação exijam de forma mais eficaz o comprometimento da equipe, bem como a análise da matéria-prima segundo as regulamentações de controle microbiológico. Além disso, a implementação de normas mais rígidas e o melhor controle da matéria-prima e das formulações finais fazem com que a qualidade dos produtos manipulados pelas farmácias magistrais seja aumentada significativamente, favorecendo o consumidor na efetiva finalidade a que o produto objetiva atingir.

Development and optimization of metoclopramide containing polymeric patches: impact of permeation enhancers

Abstract The study is aimed to develop a monolithic controlled matrix transdermal patches containing Metoclopramide as a model drug by solvent casting method. Eudragit L100, Polyvinylpyrrolidone K-30, and Methylcellulose were used in different ratios and Polyethylene glycol 400 added as a plasticizer. Resulting patches were evaluated for their physicochemical characters like organoleptic characters, weight variation, folding endurance, thickness, swelling index, flatness, drug content, swelling index, percentage erosion, moisture content, water vapor transmission rate and moisture uptake. Formed patches were also evaluated through Fourier transform spectroscopy (FT-IR), X-ray diffraction (XRD), Differential Scanning calorimetry (DSC) and Scanning Electron Microscopy (SEM). Results of SEM unveiled smooth surface of drug-loaded patches. In-vitro dissolution studies were conducted by using dissolution medium phosphate buffer saline pH 7.4. Effect of natural permeation enhancers was elucidated on two optimized formulations (Z4 and Z9). Different concentrations (5%-10 %) of permeation enhancers i.e. Olive oil, Castor oil and Eucalyptus oil were evaluated on Franz diffusion cell using excised abdominal rat skin. Z4-O2 (Olive oil 10%) had enhanced sustain effect and flux value (310.72) close to the desired flux value. Z4-O2 followed Higuchi release model (R2= 0.9833) with non-fickian diffusion release mechanism (n=0.612)

In vitro skin retention and drug permeation study of Tongluo-Qutong rubber plaster by UPLC/UV/MS/MS

Abstract Tongluo-Qutong rubber plaster (TQRP), a typical Chinese patent medicine that contains 13 different herbal remedies, is widely used in clinical practice for the treatment of cervical spondylosis and osteoarthritis. However, due to a lack of in vitro transdermal studies, the active ingredients of TQRP have not been fully elucidated. This presents a huge obstacle for quality evaluation, pharmacokinetic studies and clinical safety assessment of TQRP. In this work, a UPLC/UV/MS/MS method was established and validated to evaluate five analytes in TQRP. The validation demonstrated linearity (r > 0.99), specificity (no co-eluting peaks at the retention times of the analytes), and precision (RSD < 15%) within acceptable parameters. A skin permeation study was performed to determine the concentrations of drugs delivered to the dermis. The 24-hour cumulative permeation of ferulic acid, aleo-emodin, emodin and piperine were 303.68, 709.31, 671.06 and 25561.01 ng/cm2, respectively. According to the fitting data of the TQRP active components, skin permeation was mainly due to a combination of passive diffusion and drug release after matrix erosion

Challenges of nanotechnology in cosmetic permeation with caffeine

Abstract The evolution of beauty market and personal care is constant in Brazil as well in the rest of the world. Technological advances have brought up nanotechnology to the cosmetological field, employing active principles at atoms enveloped by vesicles, in order to take the active principle precisely to the target tissue to optimize the results achieved because of the considerable ease to cross skin barriers. Manufacturing of nanotechnology cosmetics is confronted with low absorption capacity. One of the many active principle found in cosmetic industry is caffeine, a pseudoalkaloid from the xanthine group used as a stimulant with the mechanism of the lipolytic action. This active is widely used in a esthetics and cosmetics field in treatments involving dysfunctions such as localized fat and fibroedema geloid. To work out perfectly, the principle active need to interact and create a set of factors that includes lipolysis intensification. The caffeine encapsulation in gel-based nanocosmetics has the purpose of taking this active up to the adipocyte, the target cell, for mentioned dysfunctions treatment. Thus, we aim to present a review of how has been, the use of caffeine in the production of cosmetics.

Resumo A evolução do mercado de beleza e cuidados pessoais é constante no Brasil e no resto do mundo. Os avanços tecnológicos trouxeram a nanotecnologia para o campo cosmetológico, empregando princípios ativos em átomos envolvidos por vesículas, a fim de levar o princípio ativo precisamente ao tecido alvo para otimizar os resultados alcançados devido à considerável facilidade de atravessar barreiras cutâneas. A fabricação de cosméticos nanotecnológicos é confrontada com baixa capacidade de absorção. Um dos muitos princípios ativos encontrados na indústria cosmética é a cafeína, um pseudoalocalóide do grupo xantina usado como estimulante no mecanismo da ação lipolítica. Este ativo é amplamente utilizado no campo da estética e dos cosméticos em tratamentos que envolvem disfunções, como gordura localizada e fibroedema gelóide. Para funcionar perfeitamente, o princípio ativo precisa interagir e criar um conjunto de fatores que inclui a intensificação da lipólise. O encapsulamento de cafeína em nanocosméticos à base de gel tem o objetivo de levar esse ativo até o adipócito, a célula alvo, para o tratamento de disfunções mencionado. Assim, objetivamos apresentar uma revisão de como tem sido o uso de cafeína na produção de cosméticos.

Quality of cosmetics with active caffeine in cream and gel galenic bases prepared by compounding pharmacies

Abstract As there is a great scarcity of studies on the importance of good compounding practices in the preparation of cosmetics, this study aimed to evaluate the quality control of cosmetics with active ingredient caffeine for the treatment of cellulite prepared by magistrals pharmacies. Microbiological analyzes, pH determination, color measurement, quantification of the percentage of the active ingredient caffeine and viscosity in creams and gels with 5% of the active ingredient caffeine were performed. In the microbiological analysis, the presence of molds and yeasts was verified above the permitted level according to the Brazilian pharmacopoeia. The pH decreased over time, contributing to the formulations becoming more acidic. In the color parameters, it was found that pharmacy F4 showed a brownish color, both for the gel and for the cream. The percentage of caffeine was within specifications in all formulations and the viscosity remained unchanged during the shelf life of the samples. It is important that the compounding pharmacies demand more effectively the commitment of the team, as well as the analysis of the raw material according to the microbiological control regulations to translate into the quality of the products prepared by the pharmacies and favor the consumer in the effective objective that the product you want to achieve.

Resumo Como há uma grande escassez de estudos sobre a importância de boas práticas de manipulação na elaboração de cosméticos, o presente estudo teve como objetivo avaliar o controle de qualidade de cosméticos com princípio ativo cafeína para o tratamento de celulite, elaborados por farmácias de manipulação de Campo Mourão. Foram realizadas análises microbiológicas, determinação do pH, mensuração da coloração, quantificação da porcentagem do princípio ativo cafeína e viscosidade em cremes e geís com 5% do princípio ativo cafeína. Nas análises microbiológicas foi verificada a presença de bolores e leveduras acima do pemitido segundo a farmacopéia brasileira. O pH diminuiu ao longo do tempo, contribuindo para que as formulações ficassem mais ácidas. Nos parâmetros de cor averiguou-se que a farmácia F4 apresentou uma coloração amarronzada, tanto para o gel quanto para o creme. A porcentagem de cafeína estava dentro das especificações em todas as formulações e a viscosidade se manteve inalterada durante o prazo de validade das amostras. Com o propósito de um melhor preparo magistral é importante que as farmácias de manipulação exijam de forma mais eficaz o comprometimento da equipe, bem como a análise da matéria-prima segundo as regulamentações de controle microbiológico. Além disso, a implementação de normas mais rígidas e o melhor controle da matéria-prima e das formulações finais fazem com que a qualidade dos produtos manipulados pelas farmácias magistrais seja aumentada significativamente, favorecendo o consumidor na efetiva finalidade a que o produto objetiva atingir.

An overview of preparation and characterization of solid binary system and its application on transdermal film with variation of plasticizers

Chemotherapy induced nausea and vomiting (CINV) and post-operative nausea and vomiting (PONV) is a problem, often occurs in patient. Inspite of high bioavailability, the demerits such as: hepatic first pass metabolism and invasive nature of oral and parenteral dosage forms can be avoided with anti-emetic therapy of transdermal device. The major objective of the present study is to modify the hydrochloride (HCl) form of Ondansetron (OND) to the base form followed by improvement of solubility and permeability of OND by employing solid dispersion (SD) loaded patches. Preformulation study, as observed, begins with an approach to enthuse solubility of OND by SD technique choosing different carriers. The choice of carriers was rationalized by phase solubility study. Several combinations of transdermal films were prepared with pure drug, carriers and SDs with plasticizer Ka values of OND-HPßCD binary system were found lower (54.43 to 187.57 M-1) than that of OND-PVP K-30 binary system (1156.77 to 12203.6 M-1). The drug content of SDs and patches were found satisfactory. Better permeation rate (236.48±3.66 µg/3.935 cm2) with promising flux enhancement (8.30 fold) was found with DBP loaded SD patch (P6*). Hence, enhancement of solubility and permeability of P6* ensures that it can successfully enhance the bioavailability

Quality of cosmetics with active caffeine in cream and gel galenic bases prepared by compounding pharmacies / Qualidade de cosméticos com cafeína ativa em bases galênicas em creme e gel preparadas por farmácias de manipulação

As there is a great scarcity of studies on the importance of good compounding practices in the preparation of cosmetics, this study aimed to evaluate the quality control of cosmetics with active ingredient caffeine for the treatment of cellulite prepared by magistrals pharmacies. Microbiological analyzes, pH determination, color measurement, quantification of the percentage of the active ingredient caffeine and viscosity in creams and gels with 5% of the active ingredient caffeine were performed. In the microbiological analysis, the presence of molds and yeasts was verified above the permitted level according to the Brazilian pharmacopoeia. The pH decreased over time, contributing to the formulations becoming more acidic. In the color parameters, it was found that pharmacy F4 showed a brownish color, both for the gel and for the cream. The percentage of caffeine was within specifications in all formulations and the viscosity remained unchanged during the shelf life of the samples. It is important that the compounding pharmacies demand more effectively the commitment of the team, as well as the analysis of the raw material according to the microbiological control regulations to translate into the quality of the products prepared by the pharmacies and favor the consumer in the effective objective that the product you want to achieve.

Como há uma grande escassez de estudos sobre a importância de boas práticas de manipulação na elaboração de cosméticos, o presente estudo teve como objetivo avaliar o controle de qualidade de cosméticos com princípio ativo cafeína para o tratamento de celulite, elaborados por farmácias de manipulação de Campo Mourão. Foram realizadas análises microbiológicas, determinação do pH, mensuração da coloração, quantificação da porcentagem do princípio ativo cafeína e viscosidade em cremes e geís com 5% do princípio ativo cafeína. Nas análises microbiológicas foi verificada a presença de bolores e leveduras acima do pemitido segundo a farmacopéia brasileira. O pH diminuiu ao longo do tempo, contribuindo para que as formulações ficassem mais ácidas. Nos parâmetros de cor averiguou-se que a farmácia F4 apresentou uma coloração amarronzada, tanto para o gel quanto para o creme. A porcentagem de cafeína estava dentro das especificações em todas as formulações e a viscosidade se manteve inalterada durante o prazo de validade das amostras. Com o propósito de um melhor preparo magistral é importante que as farmácias de manipulação exijam de forma mais eficaz o comprometimento da equipe, bem como a análise da matéria-prima segundo as regulamentações de controle microbiológico. Além disso, a implementação de normas mais rígidas e o melhor controle da matéria-prima e das formulações finais fazem com que a qualidade dos produtos manipulados pelas farmácias magistrais seja aumentada significativamente, favorecendo o consumidor na efetiva finalidade a que o produto objetiva atingir.