Abstract
The objective of this work was to prepare Fluconazole nanoparticles, and then incorporated into the freshly prepared gel for transdermal delivery, reducing the oral side effects of the drug and forenhancing stability. Fluconazole is commonly used antifungal agents for the treatment of local and systemic fungal infections. In this study Fluconazole nanoparticles was prepared by using Eudragit RL 100 by nanoprecipitation method with different drugs to polymer (1:1, 1:2 and 1:3) and stabilizer (Poloxamer 188) ratios (0.5%, 0.75% and 1%) and evaluated for various parameters. Drug-excipients compatibility was performed by FTIR study. The particle size, polydispersity index, Zeta potential, % Entrapment efficiency and % drug content of all the formulations were found in the range of 16.8 to 48.9nm, 0.229 to 0.558, -11.6 to -26.6 mv, 28.41% to 95.78% and 59% to 97.38%. From SEM studies it was revealed that Fluconazole nanoparticles particles are spherical in shape and without any agglomeration. From the in-vitro drug release study, it was revealed that sustained release of same formulation last up to 12 hours. From the stability study, it was revealed that the F5 formulation was stable at 40°C ± 2°C /75% ± 5%RH and 4°C. The optimised formulation F5 was selected to prepare Fluconazole loaded nanoparticles based topical gels using different concentration of Carbopol 934 and 940 and characterized for pH, spreadability, drug content, viscosity and in-vitro drug diffusion. Among the five formulations, G5 was selected as the best formulation. The pH of all formulations was found near to the skin pH value. The in-vitrodiffusion study of Fluconazole gel (G5) showed 94.75%. The optimized formulation G5 was checked for mechanism and kinetics of drug release. It is found it following Zero order release and non-Fickian mechanism. The selected Gel formulation G5 was found to be stable at 40°C ± 2°C /75% ± 5%RH and 4°C, it is clear that the formulation did not undergo any chemical changes found more stable at room temperature
Highlights
Topical or transdermal drug delivery is challenging because the skin acts as a natural protective barrier
The internal organic phase solutions were slowly injected at the rate of (1ml/minute) into the external aqueous solution containing stabilizing agent (Poloxamer 188) at various concentrations in double distilled water, and the mixtures were stirred at 500 rpm for 4 hours at room temperature
The results showed no significant difference in the particle size, polydispersity index, zeta potential, entrapment efficiency, drug content and cumulative drug release
Summary
Topical or transdermal drug delivery is challenging because the skin acts as a natural protective barrier. Several methods have been examined to increase the permeation of therapeutic molecules into and through the skin and one such approach is the use of Nanoparticulate delivery system. Drug delivery from colloidal systems such as nanoparticles dispersed in a gel appears to be unique when compared to the delivery from traditional topical and dermatological formulations. The transdermal drug delivery system can be used to deliver antifungal drug across the skin for the treatment of dermatological disease as well as skin care. Fungal infections are very common in human beings, especially in the tropical regions. Fungi produce a wide spectrum of human infections ranging from superficial skin infections affecting the outer layers of skin, hair, nails and mucous membranes to systemic infections (internal organ invasion).
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