International journal of pharmaceutics
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Comparative Study
Development of a vaginal delivery film containing EFdA, a novel anti-HIV nucleoside reverse transcriptase inhibitor.
The aim of this work was to develop a fast-dissolving film formulation containing EFdA for potential use as a topical vaginal microbicide for prevention of HIV sexual transmission. Solid state compatibility approaches were used to screen commonly used polymers for formulation development. Factorial design and desirability function were used to investigate the effect of two variables, the ratio of the polymers and the concentration of selected plasticizer on four mechanical responses including tensile strength, elongation at break, toughness and elastic modulus for optimization of the film formulation. ⋯ The results of in vitro cytotoxicity and bioactivity testing showed that 50% cytotoxic concentration (CC50) was several orders of magnitude higher than 50% effective concentration (EC50) of EFdA. Furthermore, epithelial integrity study showed that EFdA-loaded film had a much lower toxicity to HEC-1A cell monolayers as compared to VCF(®). Therefore, EFdA-loaded vaginal film may be considered as a promising vaginal microbicide for HIV prevention.
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Polyamidoamine (PAMAM) dendrimers were evaluated as nanocarriers for pulmonary delivery of the model poorly soluble anti-asthma drug beclometasone dipropionate (BDP) using G3, G4 and G4(12) dendrimers. BDP-loaded dendrimers were characterized for drug solubility, in vitro drug release and aerosolization properties using three nebulizers: Pari LC Sprint (air-jet), Aeroneb Pro (actively vibrating-mesh) and Omron MicroAir (passively vibrating-mesh) nebulizers. Solubilization of BDP using dendrimers was increased by increasing the dendrimer generation and by using higher pH media. ⋯ The "fine particle fraction (FPF)" of the aerosols was in the following order: Pari (air-jet)>Aeroneb Pro (active mesh)>Omron (passive mesh). This study demonstrates that BDP-dendrimers have potential for pulmonary inhalation using air-jet and vibrating-mesh nebulizers. Moreover, the aerosol characteristics are influenced by nebulizer design rather than dendrimer generation.