Semisolid formulations based on solid-in-oil-in-water systems containing proteins

Abstract In recent years, improvements have been made, through biotechnological processes, in the production and development of peptides capable of increasing collagen and elastin synthesis for anti-aging skin care. However, proteins have many limitations due to their structural, chemical and physical fragility to external aggressions, which may cause conformational changes, leading to loss of biological activity. Therefore, it is important to create delivery systems that protect these biomolecules from damage, allowing them to reach their target. This work aimed to develop a system able to carry bovine serum albumin (BSA), used as a model of a protein, and to incorporate this system in a semisolid formulation suitable for skin application. A microemulgel based on a solid-in-oil-in-water (S/O/W) microemulsion was prepared. Firstly, the association efficiency (AE) of lyophilized BSA-sucrose ester complex and the size of S/O nanodispersion were assessed; then, the characterization and stability evaluation of the final semisolid formulation through evaluation of pH, texture and rheological behavior were performed. The average value of AE was 54.74% ± 2.17. It was possible to develop an S/O/W microemulsion, which allowed the subsequent development of an S/O/W microemulgel that assured suitable pH, texture and rheological characteristics for skin application.

The gelling properties of Dillenia indica mucilage in benzyl benzoate emulgel formulations

Abstract The objective of the study was to evaluate the gelling properties of Dillenia indica mucilage in benzyl benzoate emulgel formulation. Mucilage was extracted from the fruits of Dillenia indica using established methods and characterized by rheology and swelling. Emulsion (F1) was prepared using the continental emulsification method. Gelling agents (2 %w /v) were prepared by dispersing in distilled water with constant stirring at a moderate speed using a magnetic stirrer. F1 was added to the gel (0-75 %w /w) to obtain emulgel formulations and evaluated using viscosity, globule size, pH, release profiles and kinetic modeling. Data were expressed as mean ± SD, and similarity factor (f2) was used to compare all formulations. Formulation viscosity was significantly higher with carbopol than with Dillenia; globule sizes increased with concentration of gelling agents, and pH reduced as the concentration of Dillenia increased. All formulations showed controlled release properties with t80 ranging between 114 and 660 min. The release was governed by Korsmeyer-Peppas model. Formulation F5 prepared with 50 % Dillenia showed highest similarity to F4 prepared with 75 %w /w carbopol. Dillenia indica demonstrated acceptable gelling properties comparable with that of carbopol and could be improved for use in emulgel formulations.

Formulation Optimization And Evaluation Of Flurbiprofen Emulgel

Objective: The objective of the present study was to formulate flurbiprofen (FLB) emulgel, evaluation of the formulations and the selection of an optimized formulation through in vitro drug release and drug content studies. Flurbiprofen is a non-steroidal anti-inflammatory drug (NSAID) requiring frequent administration and its chronic intake can lead to systemic side effects like gastric irritation and GI bleeding. The development of a dermal drug delivery system can overcome these side effects. Methods: The emulgel formulations were produced using different combinations of oil and emulsifying agents. Carbopol 940 was used as a gelling agent. The prepared emulgels were evaluated for general appearance, pH, spreadability, extrudability, drug content, in vitro drug release, average globule size and viscosity. Results: Optimized formulation F7 showed a better in vitro drug release compared to the marketed gel preparation. The stability study for the optimized formulation was carried out at 25 °C/60 % RH for 3 mo and the emulgel was found to be stable concerning the physical appearance, pH and drug content. Conclusion: The study revolved around the formulation of emulgel containing Flurbiprofen for dermal delivery of the drug. Emulgel was formulated with the purpose to enhance the permeation of poorly water-soluble drug FLB. The study concluded that the optimized emulgel containing FLB exhibited better in vitro drug release profile compared to the marketed formulation.

Original Research Article (Experimental): Design and Development of Unani Emulgel for Vitiligo

"Background: Vitiligo is not only a cosmetic problem, but also a social and psychological problemworldwide with the prevalence rate being highest in India. Treatment is unsatisfactory in WesternSystem of Medicine. Unani System of Medicine (USM) possesses various drugs to treat vitiligo inboth topical and oral dosage forms. Safoof-e-Bars (SB) is an important powdered dosage form usedwidely to treat vitiligo, internally as Zulal. Externally as Sufl (Sediment remained after decanting thesoaked drug) is used. Babchi, a component of SB, is reported to contain psoralen, an importanttherapeutically active compounds for treating vitiligo. But as Psoralen e the active marker compound is very slightly soluble in water, so only negligible amount of it comes in zulal and most ofthe amount remains in sufl. That might be the reason for local application of sufl as recommendedby Hakeems. But clinically it is observed that application of sufl is not followed by most of thepatients, due to side effects associated with its application on skin.Objective: The present study is designed to convert Safoof-e-Bars into a more convenient and appealingnewly evolved dosage form ‘emulgel’ of same composition as of SB, so that it can be used by the patientseasily without any side effects.Materials & methods: Various batches of emulgel were prepared as preliminary batches and final batchesusing hydro-alcoholic extract of SB and different excipients in different concentrations. Preliminarybatches were formed for selecting composition and concentration of extract and excipients for finalbatches. Total eight batches (F1eF8) were prepared as final batches. Among these eight batches, batch F7was selected as final batch, which was further evaluated on various parameters. Comparative quantitative analysis was done in Zulal, Hydro-alcoholic extract of SB and emulgel using HPLC.Results: Optimized emulgel showed good result in physicochemical parameters. Highest percentage ofpsoralen was found in SB extract while lowest percentage was found in zulal. No growth of yeast andmould, and viable aerobic were found in emulgel on microbiological analysis. Emulgel was found to bestable for 3 months.Conclusion: Newly developed emulgel may be recommended with zulal instead of traditionally used suflwith zulal. In future emulgel will provide a solution for topical delivery of hydrophobic drugs and moreconvenient dosage form to apply locally."

Polymeric emulgel carrying Cinnamomum tamala extract: promising delivery system for potential topical applications

Currently, the use of natural compounds obtained from plants tremendously increased due to their promising therapeutic properties. The aim of this study was to formulate a stable emulgel formulation loaded with Cinnamomum tamala (CT) extract. The antioxidant activity of plant extract was determined by DPPH inhibition assay. The extract was successfully loaded into an emulgels using different concentrations of carbopol-940, liquid paraffin, emulsifying agents and preservatives. Preliminary stability study was performed of 17 CT emulgel formulations at accelerated temperature of 50 °C for 2-months. Organoleptic evaluation, centrifugation, globule size, pH, electrical conductivity and rheological studies were performed for a period of 90-days at different temperature including 8, 25, 40 and 40 °C ±75% RH. The CT extract showed promising antioxidant activity of about 81%. On the other hand, the CT loaded emulgel formulation displayed high physical stability at all tested conditions of temperature and time. However, slight decrease in pH and minimum increase in conductivity was observed at 40 and 40 °C±75% RH. The rheological examination of CT emulgel indicated the flow index values of all the samples kept at different temperatures were less than 1, demonstrated non-newtonian and pseudo-plastic nature of CT emulgel. Taken together, the CT emulgel formulation has been evinced to be an excellent addition in the field of topical formulations.

Development And In Vitro Evaluation Of A New Topical O/W Emulgel From Fruit Extract Of Pyrus Communis

Objective: The aim of the present study was to develop a new topical dosage form containing Pyrus communis fruit extract. Developed formulation was O/W Emulgel which was evaluated by its in vitro tests and its stability studies at different storage conditions. Methods: Hydroalcoholic Pyrus communis extract was prepared by the maceration process. A 4% Pyrus communis emulgel was prepared by the combination of emulsion and gel at a specific temperature and mixing through homogenizers. The formulations having different concentration of carbopol 940 (gelling agent) were placed at 8 °C, 25 °C, 40 °C and 40 °C+75%RH for 3 mo in order to find out the most stable formulation. After the selection of final emulgel formulation was eventually further evaluated for in vitro studies such as phase separation, centrifugation, rheology, pH, conductivity, organoleptic properties and mean droplet size over a period of 12 w at 8 °C, 25 °C, 40 °C and 40 °C+75%RH. Results: In vitro evaluation of the selected Pyrus communis emulgel formulation showed good resistance to phase separation on centrifugation, conductivity gradually increases due to oil in water emulgel and pH of formulation was gradually decreased. The rheological behavior was non-Newtonian pseudoplastic and showed shear thinning fluid behavior. Mean droplet size of Pyrus communis emulgel was 16.0±0.20 µm and after 90 d droplet size was 16.7±0.55 µm at high storage temperatures at 40 °C and 40 °C+75RH and no significant changes were observed at normal storage conditions at 8 °C and 25 °C. Conclusion: Pyrus communis emulgel fresh fruit extract showed stable formulation at different storage conditions. This new formulation will be a good addition to pharmaceutical dosage forms made from traditionally used plants.

Study of capsaicin emulgel on in vitro transdermal permeation, analgesic actions, and irritation / 中草药

Objective: To prepare capsaicin emulgel and investigate its transdermal delivery ability in vitro, analgesic effect and skin irritation. Methods: The effect of different penetration enhancers on the percutaneous permeation of emulgel in vitro was investigated by using the modified Franz diffusion cell. The optimal prescription was determined and the transdermal absorption of capsaicin emulgel was investigated; Analgesic effect was tested by hot plate method; The rabbit skin irritation test was used to evaluate the safety of capsaicin emulgel. Results: Peppermint oil, eucalyptus oil, and azone three kinds of penetration enhancers had no significant effect on enhancing permeation effect, so the final formulation of the emulgel was optimized without penetration enhancers. In vitro transdermal test showed that the cumulative permeation quantity of commercially available creams, self-made gels and emulgel was 18.98%, 37.04%, and 54.75%, respectively. In the hot plate method, the inhibitory rates of commercially available creams and high dose of emulgel after oral administration of 30, 60, and 90 min were 14.07%, 14.49%, 16.81%, 18.63%, 22.50%, and 25.57%. The skin irritation test results indicated that emulgel has no irritation to the rabbit skin. Conclusion: Capsaicin emulgel has good percutaneous permeability without skin irritation, the middle and high dose of emulgel have good analgesic activity, which will supply evidence for the selection for the local transdermal formulations of capsaicin.

Analysis of the effect of psychological intervention combined with Votalin emulgel and dexamethasone sticking on the treatment of acute gouty arthritis / 中国生化药物杂志

Objective To study the effect of psychological intervention combined with Votalin emulgel and dexamethasone sticking on the treatment of acute gouty arthritis. Methods 100 patients with acute gouty arthritis treated in our hospital from March 2015 to May 2016 were selected as the research object. They were randomly divided into the control group and the experimental group, with 50 patients in each group. The control group was treated with conventional therapy, the experimental group was treated with psychological intervention combined with Votalin emulgel and dexamethasone sticking, pay attention to the psychological status of patients, strengthen communication and exchanges with patients, the patient's confidence and treatment compliance. The therapeutic effects of the experimental group and the control group were compared and analyzed. Results After the corresponding treatment, the effective rate of the experimental group was 94.0%, which was significantly higher than that of the control group (80.0%), the difference was statistically significant (P<0.05). The remission time of gout in the control group was (12.19±1.56) days,significantly longer than that in the experimental group (9.34±1.21) days, the difference was statistically significant (P<0.05). Conclusion The clinical effect of paste dressing in the treatment of acute gouty arthritis with good psychological intervention combined with Votalin emulgel, dexamethasone, relieve the clinical symptoms of patients with gout, has clinical significance.

Analysis of the effect of psychological intervention combined with Votalin emulgel and dexamethasone sticking on the treatment of acute gouty arthritis / 中国生化药物杂志

Objective To study the effect of psychological intervention combined with Votalin emulgel and dexamethasone sticking on the treatment of acute gouty arthritis. Methods 100 patients with acute gouty arthritis treated in our hospital from March 2015 to May 2016 were selected as the research object. They were randomly divided into the control group and the experimental group, with 50 patients in each group. The control group was treated with conventional therapy, the experimental group was treated with psychological intervention combined with Votalin emulgel and dexamethasone sticking, pay attention to the psychological status of patients, strengthen communication and exchanges with patients, the patient's confidence and treatment compliance. The therapeutic effects of the experimental group and the control group were compared and analyzed. Results After the corresponding treatment, the effective rate of the experimental group was 94.0%, which was significantly higher than that of the control group (80.0%), the difference was statistically significant (P<0.05). The remission time of gout in the control group was (12.19±1.56) days,significantly longer than that in the experimental group (9.34±1.21) days, the difference was statistically significant (P<0.05). Conclusion The clinical effect of paste dressing in the treatment of acute gouty arthritis with good psychological intervention combined with Votalin emulgel, dexamethasone, relieve the clinical symptoms of patients with gout, has clinical significance.

Recent Advances in Topical Gel Formulation.

Transdermal drug delivery systems are a constant source of interest because of the benefits that they afford in overcoming many drawbacks associated with other modes of drug delivery (i.e. oral, intravenous). Topical gels are becoming more popular due to ease of application and better precutaneous absorption. Gels are semisolid formulations, which have an external solvent phase, may be hydrophobic or hydrophilic in nature, and are immobilized within the spaces of a three-dimensional network structure. Gel formulations provide better application property and stability in comparison to cream and ointments. Skin is one of the most extensive and readily accessible organs on human body for topical administration and is main route of topical drug delivery system. Topical gels are intended for skin application or to certain mucosal surfaces for local action or percutaneous penetration of medicament or for their emollient or protective action. Recent studies have reported other types of gels for dermal drug application, such as proniosomal gels, emulgels, bigels and aerogels. This review is concern with all detail information regarding novel approaches to topical gel formulation, advantages and classification of gel.

Formulation and Evaluation of Optimized Clotrimazole Emulgel Formulations.

Aims: The aim of the present study was to develop an emulgel formulation of Clotrimazole using carbopol 934 or hydroxyl propyl methyl cellulose 2910 as a gelling agent. The influence of the type of gelling agent and the concentration of both the oil phase and the emulsifying agent on the release of the drug and its microbial activity were investigated using 23 factorial designs. In addition, rheological properties were also evaluated. Methodology: Within the major group of semisolid preparations, emulgel has emerged as a promising drug delivery system for the delivery of hydrophobic drugs. Different emulgel formulations were optimized using a 23 factorial design considering three independent factors at two levels; gelling agent (carbopol 934 and hydroxyl propyl methyl cellulose, liquid paraffin (2.5% and 5%) and emulsifying agent (1.5 and 2.5%). The amount of drug released (Y1) and the antifungalactivity (Y2) were chosen as two dependent responses. The prepared emulgel were also evaluated for their physical properties, pH, drug content and rheological properties. Results: The prepared emulgel exhibited higher release when compared with canest in cream as a market product. Rheological study revealed that the emulgel exhibited a thixotropic behavior. Candida albicans was used as a model fungus to evaluate the antifungal activity of the prepared formulations achieved using canestin cream as a control. Stability studies revealed no significant differences before and after storage for the selected formula. Conclusion: It was suggested that Clotrimazole emulgel formulation (F6) prepared using HPMC 2910 as gelling agent, emulsifying agent in its high level and liquid paraffin in its low level was the formula of choice since it showed the highest drug release and the highest antifungal activity.