Pouteria ramiflora leaf extract on emulgel in wound healing activity in diabetic rats

The genus Pouteria has been studied because it presents various activities, among which is its anti-inflammatory potential. The effects of Pouteria ramiflora Carbopol gel on the healing of skin wounds in diabetic rats were evaluated by microscopic imaging. Streptozotocin was administered intraperitoneally in animals that had fasted for 12 hours, a situation confirmed by the glycemic index (˃ 240 mg dL-1). An excision on the back of the animals was performed and three groups were formed: Control (Gel), Ethanolic extract (Ext) and Gel + extract 2% (Ext+gel); the histopathological evaluation occurred on the 7th, 14th, 21st and 30th days after the post-operative period. The results of the phytochemical prospecting of P. ramiflora extract demonstrated the major presence of phenolic compounds and flavonoids; the assessment of the inflammatory infiltrate on the 7th day was higher on group Ext and Ext+gel when compared to group Control; on the 14th day control and Ext (p<0.05). The quantification of fibroblasts was higher on the 7th day among the three treatments, control and Ext (p<0.05), on the 21st day. Angiogenesis showed a higher number of vessels in Ext+gel group (p<0.05) on the 7th day; in Control, Ext and Ext+gel (p<0.05) on the 14th day; and Control and Ext (p<0.05)on the 21st day. The histopathological results showed that the formulation Ext+gel was efficient in tissue reparation and decrease in inflammatory cells on the diabetic’s animals.

Formulation and Evaluation of Hydrogels containing Liposomes Entrapped with Antifungal Agent

Background: The main aim of the present study was to formulate and evaluate prolonged release Fluconazole liposomal gel for the transdermal delivery. Fluconazole, α-(2.4-diflurofenil)-α-(1H-triazole-1-methyl)-1H-1, 2, 4-triazole-1-ethanol, is a class of antifungal of triazole. It shows the action against species of Candida sp., and it is specified in cases of or pharyngeal candidiasis, esophageal, vaginal, and deep infection. Materials and Method: Fluconazole liposomal gel was prepared by thin film hydration method using phosphatidyl choline and cholesterol. Liposomes were characterized for entrapment efficiency, particle size, and surface charge. Liposomes were then dispersed into a Carbopol gel base to form liposomal gel and evaluated for drug content, pH, spreadability, viscosity and in-vitro drug release. Results: The results indicated that concentration of cholesterol in the formulations affected the particle size and entrapment efficiency. When the concentration of cholesterol increased particle size was also increased but decrease in entrapment efficiency. The viscosity of Fluconazole liposomal gel decreases with increasing rate of shear. Hence it was showed that with non-Newtonian flow. In-vitro diffusion studies were carried out using cellophane membrane, results showed that liposomal gel formulation F1 (91.36%) showed highest cumulative percent of drug release and formulation F8 (76.98%) showed lowest cumulative percent of drug release. Conclusion: Therefore, Fluconazole liposomal gel sustained the drug release for the longer duration, hence decreases the number of application of drugs and also improves patient compliance.

Synthesis and Characterization of Antibacterial Carbopol/ZnO Hybrid Nanoparticles Gel

This study recommends Carbopol/zinc oxide (ZnO) hybrid nanoparticles gel as an efficient antibacterial agent against different bacterial species. To this end, ZnO nanoparticles were synthesized using chemical precipitation derived from a zinc acetate solution with ammonium hydroxide as its precipitating agent under the effect of ultrasonic radiation. The synthesized ZnO nanoparticles were stabilized simultaneously in a freshly prepared Carbopol gel at a pH of 7. The chemical composition, phase identification, particle size and shape, surface charge, pore size distribution, and the BET surface area of the ZnO nanoparticles, as well as the Carbopol/ZnO hybrid Nanoparticles gel, were by XRD, SEM, TEM, AFM, DLS, Zeta potential and BET instruments. The results revealed that the synthesized ZnO nanoparticles were well-dispersed in the Carbopol gel network, and have a wurtzite-crystalline phase of spherical shape. Moreover, the Carbopol/ZnO hybrid nanoparticles gel exhibited a particle size distribution between ~9 and ~93 nm, and a surface area of 54.26 m2/g. The synthesized Carbopol/ZnO hybrid nanoparticles gel underwent an antibacterial sensitivity test against gram-negative K. pneumonia (ATCC 13883), Bacillus subtilis (ATCC 6633), and gram-positive Staphylococcus aureus (ATCC 6538) bacterial strains, and were compared with ampicillin as a reference antibiotic agent. The obtained results demonstrated that the synthesized Carbopol/ZnO hybrid nanoparticles gel exhibited a compatible bioactivity against the different strains of bacteria.

Energy-Dependent Endocytosis Is Responsible for Skin Penetration of Formulations Based on a Combination of Indomethacin Nanoparticles and l-Menthol in Rat and Göttingen Minipig

We previously designed a Carbopol gel formulation (N-IND/MEN) based on a combination of indomethacin solid nanoparticles (IND-NPs) and l-menthol, and we reported that the N-IND/MEN showed high transdermal penetration. However, the detailed mechanism for transdermal penetration of IND-NPs was not clearly defined. In this study, we investigated whether endocytosis in the skin tissue of rat and Göttingen minipig is related to the transdermal penetration of IND-NPs using pharmacological inhibitors of endocytosis. The pharmacological inhibitors used in this study are as follows: 54 µM nystatin, a caveolae-mediated endocytosis (CavME) inhibitor; 40 µM dynasore, a clathrin-mediated endocytosis (CME) inhibitor; and 2 µM rottlerin, a micropinocytosis (MP) inhibitor. The N-IND/MEN was prepared by a bead mill method, and the particle size of solid indomethacin was 79–216 nm. In both rat and Göttingen minipig skin, skin penetration of approximately 80% IND-NPs was limited by the stratum corneum (SC), although the penetration of SC was improved by the combination of l-menthol. On the other hand, the treatment of nystatin and dynasore decreased the transdermal penetration of indomethacin in rats and Göttingen minipigs treated with N-IND/MEN. Moreover, in addition to nystatin and dynasore, rottlerin attenuated the transdermal penetration of IND-NPs in the Göttingen minipigs’ skin. In conclusion, we found that l-menthol enhanced the SC penetration of IND-NPs. In addition, this study suggests that the SC-passed IND-NPs are absorbed into the skin tissue by energy-dependent endocytosis (CavME, CME, and/or MP pathways) on the epidermis under the SC, resulting in an enhancement in transdermal penetration of IND-NPs. These findings provide significant information for the design of nanomedicines in transdermal formulations.

Collagen Hydrolysate Prepared from Chicken By-Product as a Functional Polymer in Cosmetic Formulation

Chicken stomachs can be processed into collagen hydrolysate usable in cosmetic products. The aim of the study was to verify the effects of a carbopol gel formulation enriched with 1.0% (w/w) chicken hydrolysate on the properties of the skin in the periorbital area after regular application twice a day for eight weeks in volunteers ageed 50 ± 9 years. Skin hydration, transepidermal water loss (TEWL), skin elasticity and skin relief were evaluated. Overall, skin hydration increased by 11.82% and 9.45%, TEWL decreased by 25.70% and 17.80% (always reported for the right and left area). Generally, there was an increase in skin elasticity, a decrease in skin roughness, as the resonance times decreased by 85%. The average reduction of wrinkles was 35.40% on the right and 41.20% on the left. For all results, it can be seen that the longer the cosmetic gel formulation is applied, the better the results. Due to the positive effect on the quality and functionality of the skin, it is possible to apply the cosmetic gel formulation in the periorbital area. The advantage of the product with chicken collagen hydrolysate is also the biocompatibility with the skin and the biodegradability of the formulation.

Preparation and evaluation of an oral mucoadhesive gel containing nystatin-loaded alginate microparticles

Nystatin is an antifungal agent used for prophylaxis and treatment of candidiasis, especially oral mycosis. Efficacy of nystatin conventional dosage forms is limited by the short residence time and bitter taste of the drug. This research aims at designing an optimized formulation of oral mucoadhesive gel of nystatin-loaded alginate microparticles, which can be retained in the mouth. Sodium alginate solution containing nystatin was added to the solution of calcium chloride under stirring. Microparticles containing nystatin were incorporated into the Carbopol gel. Size, loading, and release profile and mucoadhesion were investigated. The most suitable microparticles with particle size of < 250 μm were prepared with alginate concentration of 1%(w/v), calcium chloride of 1%(w/v), drug:polymer concentration 1%, and ratio of alginate solution:calcium chloride of 1:10. This formulation showed 49.1% drug loading and 98.2% encapsulation efficiency. Carbopol 934 gel provided optimal mucoadhesive properties. Release profile proved a burst release, which can be attributed to the surface associated drug, followed by a slower sustained release phase for all microparticles. The developed system with ability to adhere to the oral mucosa has great appeal for treatment of localized infections and can mask bitter taste of the drug and be retained in the mouth for long periods.