Rubber oily liquids as transdermal and periodontal pocket drug delivery systems.

This study investigates the incorporation of block natural rubber (NR) as a viscosity-inducing agent in NR oily liquids designed for drug delivery systems. A variety of liquids, encompassing natural oils, synthetic and non-oil liquids, and a eutectic mixture, were incorporated with NR using solvent displacement technique. Successful formulations were achieved for several oily liquids, with viscosity correlating to NR concentration. Particularly, a eutectic mixture of menthol and camphor exhibited optimal viscosity by direct dissolving enabling the development of transdermal ibuprofen delivery and injectable azithromycin for periodontitis treatment. NR prolonged the release of both drugs. The extended-release ibuprofen system holds promise for transdermal applications, while the azithromycin system displayed inhibitory effects against Staphylococcus aureus, Streptococcus mutans, and Porphyromonas gingivalis, suggesting potential for periodontitis treatment. Overall, this investigation advances the development of NR oily liquids as a versatile drug delivery system that can be applied both on the skin and for the local injection into the periodontal pocket, showcasing promise for various therapeutic applications.

Plant leaf mucilage/carrageenan/Eudragit® NE30D blended films: Optimization, characterization, and pharmaceutical application.

Mucilage of C. pareira leaves was utilized, being manufactured for use in pharmaceutical products. Carrageenan and Eudragit® NE30D were used to combined. Glycerin was used as a plasticizer at a concentration of 20 % w/w based on the amount of polymer used. Computer software optimized its characteristics, including tensile properties, moisture uptake, and erosion; the optimal formulation was 1.4:1.2:2.8. The percentages of optimization error ranged from 8.48 to 13.80 %. Propranolol HCl was mixed to an optimal formulation. The film layer was tight, homogeneous, and smooth, with no holes. DSC thermogram showed no interaction peaks at 101.33 °C and 170.50 °C. Propranolol HCl concentration in the film ranged from 2.18 to 2.20 mg/cm2. Propranolol HCl was quickly released from the film. The kinetic model for the release profile was first-order kinetic. Although propranolol HCl had a high-release profile, its skin permeation was limited. The permeation lag time, Jss, and Kp were 1.60-2.65 h, 0.0182-0.0338 µg/cm2/h, and 9.10-15.35 cm/h, respectively. A significant amount of propranolol HCl residue was found on the skin's surface. Glycerin appeared to influence propranolol HCl permeability. Therefore, the plant leaf mucilage/carrageenan/Eudragit® NE30D blended film can be utilized in pharmaceutical applications to control drug release from its film layer.

Evaluation of in vivo bond strength and skin irritation test for new skin adhesive.

Objectives: This study developed a new skin-deproteinized natural rubber latex (DNRL) silicone adhesive for adhering to silicone prostheses and compared the properties with a commercial Daro-Hydrobond adhesive. Materials and methods: The new DNRL skin adhesive formulation was made from non-vulcanized natural rubber-based adhesives consisting of DNRL, 20% polyvinyl alcohol, cumarone resin, 2% methylcellulose, and Wingstay L. The peel bond strength of the adhesives was tested using a 90-degree peel test. Biocompatibility was accessed using in vitro keratinocyte cell viability. Animals (rabbits) and humans were tested for skin irritation tests. Results were analyzed using SPSS Version 24 and compared between the two adhesives. Results: The peel bond strength of the new DNRL skin adhesive was 103.61 ± 23.18 N/m whereas that of the Daro-hydrobond adhesive was 131.52 ± 21.72 N/m. There was no significant difference (p>0.05) between the peel bond strengths of the two test adhesives. Cell proliferation under the DNRL skin adhesive-soaked medium showed higher cell viability than the positive control (p<0.05). The DNRL skin adhesive produced moderate erythema and edema on rabbit skins, however, the skin lesions recovered within 14 days. Two volunteers showed mild irritation at the first hour of the contact which was reduced within an hour without any therapy. The patient satisfaction with the DNRL skin adhesive ranged from slightly satisfied to completely satisfied. Conclusion: The new DNRL skin adhesive showed comparable peel bond strength and patient satisfaction to those of commercial adhesives. The adhesive was biocompatible and can be used carefully.

Porous Deproteinized Natural Rubber Film Loaded with Silver Nanoparticles for Topical Drug Delivery.

The work demonstrated the use of natural rubber for topical drug delivery. The first objective was to fabricate a porous deproteinized natural rubber film loaded with silver nanoparticles. Characterizing and assessing its formulation was the second objective. Surface pH, mechanical properties, swelling ratio, erosion, moisture vapor transmission rate, scanning electron microscopy/energy dispersive X-ray analysis, and X-ray diffraction were evaluated. In vitro studies and antibacterial activity were assessed. It was discovered that silver nanoparticles could enter the film and that their concentrations ranged between 7.25 and 21.03 µg/cm2. The pH of the film's surface was 7.00. The mechanical properties of the film with silver nanoparticle loading differed from the blank film. After adding silver nanoparticles, the film eroded faster than before, but the swelling ratio was not affected significantly. Increased time utilization had an impact on the moisture vapor transmission rate of the film. Silver nanoparticles released easily from the film while there was less permeability. The dead pig-ear skin had significant silver nanoparticle accumulation. Potent antibacterial activity was seen in the film containing silver nanoparticles. The silver nanoparticle-loaded film may be used as a wound dressing for a topical film that promotes wound healing while also protecting the area from infection.

Preparation, development, and scale-up of standardized pentacyclic triterpenoid-rich extract from Centella asiatica (L.) Urb. and study of its wound healing activity.

This pilot-scale study of an innovative green extraction method shows increased biomarker content in plant extracts. Moreover, green extraction methods decrease the effects on the environment and human health and promote industrial growth. This study optimized the process conditions to obtain a pentacyclic triterpenoid-rich extract (PRE) from Centella asiatica (L.) Urb., which contains asiatic acid, madecassic acid, asiaticoside, and madecassoside, and evaluated its biological activities. PRE preparation was scaled up from laboratory to pilot scale. In the pilot scale, a combination of microwave-assisted extraction with an irradiation power of 4 kW and an ultrasonic-assisted extraction at 0.55 kW was used for C. asiatica extraction. The total pentacyclic triterpene content was 106.02 mg/g of crude extract. Then, the C. asiatica extract was fractionated by a macroporous resin (Diaion® HP-20). The PRE preparation method used 50% and 75% EtOH fractions. This PRE produced a high content of pentacyclic triterpenoids at 681.12 mg/g of crude extract. It presented a high anti-inflammatory effect with an IC50 value of 23.88 µg/mL for nitric oxide inhibition and induced wound healing processes (proliferation, migration, and collagen synthesis) in human dermal fibroblast cells. The information gained from this study can advance the industrial extraction of physiologically active substances from various plant sources for use as medicines or components of supplemental food and cosmeceutical products.

Moxifloxacin HCl-Incorporated Aqueous-Induced Nitrocellulose-Based In Situ Gel for Periodontal Pocket Delivery.

A drug delivery system based on an aqueous-induced in situ forming gel (ISG) consists of solubilizing the drug within an organic solution of a polymer using a biocompatible organic solvent. Upon contact with an aqueous medium, the solvent diffuses out and the polymer, designed to be insoluble in water, solidifies and transforms into gel. Nitrocellulose (Nc), an aqueous insoluble nitrated ester of cellulose, should be a promising polymer for an ISG using water induction of its solution to gel state via phase inversion. The aim of this investigation was to develop and evaluate a moxifloxacin HCl (Mx)-incorporated aqueous-induced Nc-based ISG for periodontitis treatment. The effects of different solvents (N-methyl pyrrolidone (NMP), DMSO, 2-pyrrolidone (Py), and glycerol formal (Gf)) on the physicochemical and bioactivity properties of the ISGs were investigated. The viscosity and injection force of the ISGs varied depending on the solvent used, with Gf resulting in higher values of 4631.41 ± 52.81 cPs and 4.34 ± 0.42 N, respectively. All ISGs exhibited Newtonian flow and transformed into a gel state upon exposure to the aqueous phase. The Nc formulations in DMSO showed lower water tolerance (12.50 ± 0.72%). The developed ISGs were easily injectable and demonstrated water sensitivity of less than 15.44 ± 0.89%, forming a gel upon contact with aqueous phase. The transformed Nc gel effectively prolonged Mx release over two weeks via Fickian diffusion, with reduced initial burst release. Different solvent types influenced the sponge-like 3D structure of the dried Nc ISGs and affected mass loss during drug release. Incorporating Nc reduced both solvent and drug diffusion, resulting in a significantly narrower zone of bacterial growth inhibition (p < 0.05). The Mx-incorporated Nc-based ISGs exhibited efficient antibacterial activity against four strains of Staphylococcus aureu and against periodontitis pathogens including Aggregatibacter actinomycetemcomitans and Porphyromonas gingivalis. This study suggests that the developed Mx-incorporated Nc-based ISGs using DMSO and NMP as the solvents are the most promising formulations. They exhibited a low viscosity, ease of injection, and rapid transformation into a gel upon aqueous induction, and they enabled localized and prolonged drug release with effective antibacterial properties. Additionally, this study represents the first reported instance of utilizing Nc as the polymer for ISG. Further clinical experiments are necessary to evaluate the safety of this ISG formulation.

Box-Behnken design to optimize the cross-linked sodium alginate/mucilage/Aloe vera film: Physical and mechanical studies.

The crosslinked sodium alginate/mucilage/Aloe vera/glycerin was optimized by different ratios of each factor to be an absorption wound dressing base for infected wound healing. Mucilage was extracted from seeds of Ocimum americanum. The Box-Behnken design (BBD) in response surface methodology (RSM) was used to construct an optimal wound dressing base with the target ranges of mechanical and physical properties of each formulation. The independent variables selected were sodium alginate (X1: 0.25-0.75 g), mucilage (X2: 0.00-0.30 g), Aloe vera (X3: 0.00-0.30 g), and glycerin (X4: 0.00-1.00 g). The dependent variables were tensile strength (Y1: low value), elongation at break (Y2: high value), Young's modulus (Y3: high value), swelling ratio (Y4: high value), erosion (Y5: low value), and moisture uptake (Y6: high value). The results showed that the wound dressing base with the most desirable response consists of sodium alginate (59.90 % w/w), mucilage (23.96 % w/w), and glycerin (16.14 % w/w) without Aloe vera gel powder (0.00 % w/w).

Lincomycin HCl-Loaded Borneol-Based In Situ Gel for Periodontitis Treatment.

Solvent exchange-induced in situ forming gel (ISG) has emerged as a versatile drug delivery system, particularly for periodontal pocket applications. In this study, we developed lincomycin HCl-loaded ISGs using a 40% borneol-based matrix and N-methyl pyrrolidone (NMP) as a solvent. The physicochemical properties and antimicrobial activities of the ISGs were evaluated. The prepared ISGs exhibited low viscosity and reduced surface tension, allowing for easy injection and spreadability. Gel formation increased the contact angle on agarose gel, while higher lincomycin HCl content decreased water tolerance and facilitated phase separation. The drug-loading influenced solvent exchange and matrix formation, resulting in thinner and inhomogeneous borneol matrices with slower gel formation and lower gel hardness. The lincomycin HCl-loaded borneol-based ISGs demonstrated sustained drug release above the minimum inhibitory concentration (MIC) for 8 days, following Fickian diffusion and fitting well with Higuchi's equation. These formulations exhibited dose-dependent inhibition of Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 8739, and Prophyromonas gingivalis ATCC 33277, and the release of NMP effectively inhibited Candida albicans ATCC 10231. Overall, the 7.5% lincomycin HCl-loaded 40% borneol-based ISGs hold promise as localized drug delivery systems for periodontitis treatment.

Influence of talc and hydrogenated castor oil on the dissolution behavior of metformin-loaded pellets with acrylic-based sustained release coating.

Multi-unit pellet system (MUPS) is of great interest as it is amenable to customization. MUPS comprises multi-particulates, usually as pellets or spheroids, which can be coated with diffusion barrier coatings. One commonly used diffusion barrier coating is the methacrylic acid copolymer, which can be used as a taste masking, enteric or sustained release polymer. While the versatility of methacrylic acid copolymers makes them pliable for pellet coating, there are impediments associated with their use. Additives commonly required with this polymer, including plasticizer and anti-adherent, have been shown to weaken the film strength. The objective of this study was to investigate the impact of osmotic pressure within the core on the sustained release coat integrity and functionality. Hydrogenated castor oil (HCO) was chosen as the additive to be studied. Metformin-loaded pellets, prepared via extrusion-spheronization, were coated with ethyl acrylate and methyl methacrylate copolymer (Eudragit RS 30 D) containing talc, talc-HCO, or HCO to different coat thicknesses. Drug release was investigated using the USP dissolution apparatus 2 and an ultraviolet imager. The swelling of the pellets when wetted was monitored by video imaging through a microscope. When coated to 7.5 % coat weight gain, coats with HCO slowed down drug release more than the other pellets. The pellets also swelled the most, which suggests that they were more resistant to the osmotic pressure exerted by metformin. For drugs which exert high osmotic pressure, HCO can serve as an efficient alternative to talc in the preparation of methacrylic acid copolymer coatings.

Plaster Gel Loaded with Silver Nanoparticle-Mediated Ganoderma applanatum: from Fabrication to Evaluation.

Traditional Asian remedies have mainly employed the macrofungus Ganoderma applanatum, which belongs to the family Ganodermataceae, as a medicinal mushroom due to its high antibacterial and antioxidant activity. Extracts of the fungus can be synthesized into nanoparticles, which are subsequently produced as plaster gels. Synthesized silver nanoparticle-mediated G. applanatum was discovered to have the greatest ability to inhibit bacterial growth in S. epidermidis. When applied to the skin, the prepared plaster gel converted from a gel to a film; thus, both gel and film generation are characteristic of its formulation. The plaster gel that was made was found to be consistent and attractive, and the yellow color had darkened. Its viscosity and pH were appropriate for the application and allowed it to remain on the skin without dripping or reacting with the skin until it dried. A shorter duration for film formation is possible. The film's tensile was slightly reduced, and it exhibited excellent thermal stability. Decomposition of the generated film occurred at a slower rate, which constrained the polymer chain's ability to move. The semi-crystalline structure was characteristic of the film. It was found that particles were distributed in the film. Rapid release from plaster gel within 4 h was seen, and this was followed by a period of a slowly declining release rate over 12 h. The accurate first-order kinetic used to estimate the release rate of the formulation. The plaster gel demonstrated greater antibacterial activity than the MIC value indicated. The in vivo evaluation was positive and showed no skin irritation. The formulation showed good stability. Therefore, this indicated that the prepared plaster gel is appropriate for topical pharmaceutical delivery and safe for skin application.

Effect of Ionic Liquid on Silver-Nanoparticle-Complexed Ganoderma applanatum and Its Topical Film Formulation.

Imidazolium-based ionic liquids have been widely utilized as versatile solvents for metal nanoparticle preparation. Silver nanoparticles and Ganoderma applanatum have displayed potent antimicrobial activities. This work aimed to study the effect of 1-butyl-3-methylimidazolium bromide-based ionic liquid on the silver-nanoparticle-complexed G. applanatum and its topical film. The ratio and conditions for preparation were optimized by the design of the experiments. The optimal ratio was silver nanoparticles: G. applanatum extract: ionic liquid at 97:1:2, and the conditions were 80 °C for 1 h. The prediction was corrected with a low percentage error. The optimized formula was loaded into a topical film made of polyvinyl alcohol and Eudragit®, and its properties were evaluated. The topical film was uniform, smooth, and compact and had other desired characteristics. The topical film was able to control the release of silver-nanoparticle-complexed G. applanatum from the matrix layer. Higuchi's model was used to fit the kinetic of the release. The skin permeability of the silver-nanoparticle-complexed G. applanatum was improved by about 1.7 times by the ionic liquid, which might increase solubility. The produced film is suitable for topical applications and may be utilized in the development of potential future therapeutic agents for the treatment of diseases.

Natural rubber blends for floating theophylline beads.

Natural rubber (NR)'s value has become increasingly important for human applications. This study prepared NR beads as floating drug delivery system by dripping NR latex into hardening solution to obtain spherical beads. Theophylline was loaded as a model drug. NR latex formed into harden beads suddenly after dripping droplets in acidic medium. These NR beads floated instantly and buoyant in HCl buffer for over 8 h with prolonged theophylline release. Their morphologies, crystallinity and thermal properties were observed using microscope, X-ray diffractometer, and thermogravimetry, respectively. Addition of 100 phr sodium bicarbonate increased drug release owing to liberation of carbon dioxide promoting porous NR matrix. Composite of 50 and 200 phr shellac in NR beads floated in HCl buffer for over 12 h. Moreover, 200 phr shellac efficiently retarded release of theophylline from NR composite beads (lower than 10 % in 8 h), whereby promoting theophylline release in phosphate buffer (pH 6.8) (approximately 80 % in 8 h). NR-shellac beads had greater water sorption (2.5 times) and erosion (4.9 times) in phosphate buffer than in HCl buffer. Thus, NR beads exhibited desirable attributes as floating drug delivery system. Both sodium bicarbonate and shellac modified matrix properties and drug release of NR beads.

New Insight into the Impact of Effervescence on Gel Layer Microstructure and Drug Release of Effervescent Matrices Using Combined Mechanical and Imaging Characterisation Techniques.

Gel layer characteristics play a crucial role in hydrophilic hydroxypropyl methylcellulose (HPMC) matrix development. Effervescent agents have the potential to affect the gel layer microstructures. This study aimed to investigate the influence of effervescence on the microstructure of the gel layer around HPMC matrices using a combination of texture analysis and imaging techniques. The relationship with drug release profile and release mechanisms were also examined. The high amounts of effervescent agents promoted a rapid carbonation reaction, resulting in a high gel layer formation with a low gel strength through texture analysis. This finding was ascribed to the enhanced surface roughness and porosity observed under digital microscopy and microporous structure of the gel layer under scanning electron microscopy. The reconstructed three-dimensional images from synchrotron radiation X-ray tomographic microscopy notably exhibited the interconnected pores of various sizes from the carbonation reaction of effervescent and microporous networks, indicating the gel layer on the tablet surface. Notably, effervescence promoted the increase in interconnected porosities, which directly influenced the strength of the gel layer microstructure, drug release patterns and release mechanism of the effervescent matrix tablet. Therefore, combined mechanical characterisation and imaging techniques can provide new insights into the role of effervescent agents on the gel layer microstructure, and describe the relationship of drug release patterns and release mechanism of matrix tablets.

Imatinib Mesylate-Loaded Rosin/Cinnamon Oil-Based In Situ Forming Gel against Colorectal Cancer Cells.

Localized delivery systems have been typically designed to enhance drug concentration at a target site and minimize systemic drug toxicity. A rosin/cinnamon oil (CO) in situ forming gel (ISG) was developed for the sustainable delivery of imatinib mesylate (IM) against colorectal cancer cells. CO has been claimed to express a potent anticancer effect against various cancer cells, as well as a synergistic effect with IM on colorectal cancer cells; however, poor aqueous solubility limits its application. The effect of rosin with the adding CO was assessed on physicochemical properties and in vitro drug release from developed IM-loaded rosin/CO-based ISG. Moreover, in vitro cytotoxicity tests were conducted against two colorectal cancer cells. All formulations exhibited Newtonian flow behavior with viscosity less than 266.9 cP with easier injectability. The adding of CO decreased the hardness and increased the adhesive force of the obtained rosin gel. The gel formation increased over time under microscopic observation. CO-added ISG had a particle-like gel appearance, and it promoted a higher release of IM over a period of 28 days. All tested ISG formulations revealed cytotoxicity against HCT-116 and HT-29 cell lines at different incubation times. Thus, CO-loaded rosin-based ISG can act as a potentially sustainable IM delivery system for chemotherapy against colorectal cancer cells.

Fabrication and Characterization of Buccal Film Loaded Self-emulsifying Drug Delivery System containing Lysiphyllum strychnifolium Stem Extracts.

Lysiphyllum strychnifolium has long been used as a popular herbal medicinal plant for treating fever and alcohol intoxication. This study aimed to prepare buccal film for L. strychnifolium stem extracts. These extracts were less soluble in water and were therefore loaded in self-emulsifying systems before being mixed into the film. Astilbin was selected as a chemical marker in L. strychnifolium stem extracts. Firstly, the L. strychnifolium stem extracts were entrapped in the self-emulsifying systems which were designed and optimized based on 32 factorial design. The optimal formulation was 0.60 g of surfactant-co-surfactant mixture (Tween® 80 and polyethylene glycol 400 in the ratio of 7.5:1) and 0.40 g of caprylic/capric triglyceride. Secondly, the optimal self-emulsifying system was loaded in the polymeric film which consisted of polyvinyl alcohol blended with poloxamer 407 using glycerin as a plasticizer. The properties of the prepared buccal film were unchanged, and the film showed an amorphous state, indicating all ingredients might be completely dissolved in the film. The buccal film could be placed in direct contact with the mouth without oral mucosal irritation, and showed a smooth and homogeneous surface with a rough and compact cross-sectional morphology. Astilbin content in the buccal film was 61.39 ± 11.45 µg/cm2. Astilbin was released from the buccal film while the permeation rate was low. The release mechanism was both swelling and diffusion, and followed anomalous or non-Fickian transfer. The permeability coefficient of the cumulative amount of astilbin permeated from buccal film was 1.0192 ± 0.1395 ×10-3 cm/h. Thus, the buccal film can be prepared by using a self-emulsifying system for herbal applications and shows potential as a safe and convenient form of oral drug administration.

Design and optimization of process parameters of polyvinyl alcohol-graft-lactic acid films for transdermal drug delivery.

The objective was to apply a simplex lattice design to determine the properties of polyvinyl alcohol-graft-lactic acid (PVA-g-LA) with different values for two independent variables: curing time (X1) and LA ratio (X2). Each independent variable was varied among three levels: -1, 0, and +1. Three coded levels were 120 min, 150 min, and 180 min for X1 and 2.5 g, 5 g, and 7.5 g for X2. Dependent variables of swelling behavior in various swelling media and thermal analysis parameters were monitored. The optimal formulation was selected based on the desirability value. The prediction was accurate, showing a low value of percent error. The morphology of the selected formulation with the highest desirability value showed a compact and dense film. Propranolol hydrochloride used as a model drug, was loaded into PVA-g-LA film. The propranolol hydrochloride content was 4.19 ± 1.05 mg/cm2. The cumulative release and permeation of drug were 61.94 ± 8.03% and 59.96 ± 6.61%, respectively. Thus, response surface methodology can be used as a tool to predict or optimize the process parameters for PVA-g-LA transdermal films in an accurate manner. PVA-g-LA could control the release and permeation of drug from the film layer.

Transdermal patches of lidocaine/aspirin ionic liquid drug-loaded gelatin/polyvinyl alcohol composite film prepared by freeze-thawed procedure.

The objectives of this study are to prepare a 5 wt% lidocaine/aspirin ionic liquid drug-loaded gelatin/polyvinyl alcohol composite film using a freeze-thaw procedure and to evaluate their physicochemical characteristics, in vitro drug release, and stability. Lidocaine/aspirin ionic liquid drugs can be prepared by an ion-pair reaction between the hydrochloride salts of lidocaine and the sodium salts of aspirin, which showed a significant change in their thermal properties when compared to those pure drugs. The results showed that a transdermal patch could feasibly be used in pharmaceutical transdermal patches with good physicochemical properties. A chemical interaction between the drug and polymer base was not found. Decomposition of the lidocaine/aspirin ionic liquid drug was found in the patch; however, the properties of the patch were not changed after drug loading. The patch controlled the drug release and showed good stability during the studied period of three months when kept at 4°C more than at ambient temperature and 45°C.

Lidocaine loaded gelatin/gelatinized tapioca starch films for buccal delivery and the irritancy evaluation using chick chorioallantoic membrane.

The aim of this study was to confirm the feasibility of gelatin/gelatinized tapioca starch (α st) films for buccal delivery and to evaluate their irritancy. Lidocaine (LB) and lidocaine hydrochloride (LH) were used as model drugs and glycerin was used as the plasticizer. The scanning electron microscopy, atomic force electron microscopy, X-ray diffraction and thermogravimetric analysis results confirmed the compatibility of gelatin/α st/glycerin (Gαgly) films. Drug releases of LB- or LH-Gαgly films were evaluated. The drug release profiles of medicated films presented good patterns in both short time and 8 h drug release studies. The permeation study was examined through chick chorioallantoic membrane (CAM) by using modified Franz diffusion cells. Moreover, the irritancy study for buccal films was also examined by a hen's egg test on CAM model (HET-CAM). The results revealed that LB and LH could permeate through CAM, and these Gαgly films created no irritation on HET-CAM. This indicates that the LB- and LH-Gαgly films are possible to use as buccal films.

Controlled Release of Lidocaine-Diclofenac Ionic Liquid Drug from Freeze-Thawed Gelatin/Poly(Vinyl Alcohol) Transdermal Patches.

The objectives of this work were to prepare a 5 wt% lidocaine-diclofenac ionic liquid drug-loaded gelatin/poly(vinyl alcohol) transdermal patch using a freeze/thaw method and to evaluate its physicochemical properties, in vitro release of lidocaine and diclofenac, and stability test. The lidocaine-diclofenac ionic liquid drug was produced by the ion pair reaction between the hydrochloride salts of lidocaine and the sodium salts of diclofenac. The thermal properties of the final drug product were significantly changed from the primary drugs. The ionic liquid drug could be dissolved in water and mixed in a polymer solution. The resulting transdermal patch was then exposed to 10 cycles of freezing and thawing preparation at - 20°C for 8 h and at 25°C for 4 h, respectively. As a result, it was found that the lidocaine-diclofenac ionic liquid drug-loaded transdermal patch showed good physicochemical properties and could feasibly be used in pharmaceutical applications. The lidocaine-diclofenac ionic liquid drug was not affected by the properties of the transdermal patch due to the lack of chemical interaction between polymer base and drug. The high drug release values of both lidocaine and diclofenac were controlled by the gelatin/poly(vinyl alcohol) transdermal patch. The patch showed good stability over the study period of 3 months when kept at 4°C or under ambient temperature.

Comparison of Pectin Layers for Nicotine Transdermal Patch Preparation.

Purpose: The objective of the present investigation was to prepare and evaluate transdermal patches for nicotine. Methods: Pectin isolated from the hulls of Monthong durian or leaves of Krueo Ma Noy was used as a matrix membrane for the controlled release of nicotine and compared with commercial pectin. The mechanical properties, moisture uptake, and Fourier transform infrared spectra were characterized. The in vitro stability of these patches was evaluated and compared to commercial nicotine patches. Results: The mechanical properties of the patches made from isolated pectin were greater than those prepared from commercial pectin; brittle commercial patches were obtained after nicotine loading. The moisture uptake of the patches made with isolated pectin was in the range of 30.20-44.29%. There was no incompatibility between the ingredients of the nicotine transdermal patches or any degradation of the drug. The matrix layer made from isolated pectin controlled the nicotine release more effectively than did commercial nicotine patches. In addition, these patches were stable at in a refrigerator (approximately 4±2 °C) and at ambient temperature (approximately 30±2 °C) for 3 months, retaining 90% of the loaded nicotine. Conclusion: Our study suggests that using isolated pectin as the matrix layer should control the release of nicotine from transdermal patches.