No abstract

Vitamin D3 is available in oral and injectable dosage forms. Interest in the transdermal route as an alternative to the oral and parenteral routes has grown recently. In this study, several film-forming solutions for the transdermal delivery of vitamin D3 were prepared. They contained 6000 IU/mL of vitamin D3 that formed a dry and acceptable film in less than 5 min after application. The formulations consisted of ethanol and acetone 80:20, and one or more of the following ingredients: Eudragit L100-55, PVP, PG, limonene, oleic acid, camphor, and menthol. Vitamin D3 release was studied from both the film-forming solution and pre-dried films using a Franz diffusion cell. The film-forming solution released a significant amount of vitamin D3 compared to the dry film, which is attributed mostly to the saturation driving force due to the evaporation of volatile solvents. In vitro permeation studies through artificial skin Strat M® membrane revealed that the cumulative amount of vitamin D3 permeated after 24 h under the experimental conditions was around 800 IU across 3.14 cm2. The cumulative permeation curve showed faster permeation in earlier stages. Young’s modulus, viscosity, and pH of the formulations were determined. Most of the formulations were stable for 3 weeks.

The effect of various penetration enhancers on the permeation of dexchlorpheniramine maleate from a 2 wt% aqueous phase and from water/oil emulsions (creams) was studied using a modified Franz diffusion cell. A polyamide membrane filter (modeling a biomembrane) was impregnated with n-octanol, sandwiched between two dialysis membranes, and placed between the source and receiver compartments. The permeation coefficient in the aqueous phase was 270 times greater than that in the cream, while the lag time was 3.5 times longer in the cream. A mixture of isopropyl myristate and ethanol (8 : 2) gave the highest enhancement ratio, while oleic acid acted as a penetration retardant in the cream formulation.

Background: Rutin is available on the market as a topical formulation for the treatment of several conditions, such as internal bleeding, hemorrhoids, and varicose veins. However, these gels have low solubility and limited bioavailability due to their decreased lipid solubility. Objective: In this study, we aimed to synthesize potentially novel lipophilic rutin prodrugs. The suggested library of these rutin prodrugs includes changing the solubility profile to facilitate rutin transport across biological barriers, thereby improving drug delivery through topical application. Methods: Six rutin derivatives were synthesized based on the ester prodrug strategy. The synthesized compounds were formulated as topical ointments, and their permeability via Franz diffusion was measured. An ultraviolet (UV) analytical method was developed in our laboratories to quantify rutin derivatives both as raw materials and in final dosage forms. The analytical method was then validated. Result: The results of Franz diffusion analyses showed that transdermal permeability increased by 10_Fo.jpgl height=""d for decaacetylated rutin compared to the other esterified rutins. A simple analytical method for the analysis of the formulated rutin ester was developed and validated. Moreover, the formulated ointment of decaacetylated rutin in our research laboratory was found to be stable under stability accelerated conditions. Synthesis of potentially more lipophilic compounds would yield novel rutin prodrugs suitable for topical formulation. Conclusion: This project provides a synthetic approach for many similar natural products. The research idea and strategy followed in this research project could be adapted by pharmaceutical and herbal establishments.