Polymeric versus lipid nanocapsules for miconazole nitrate enhanced topical delivery: in vitro and ex vivo evaluation

Nanocapsules can be equated to other nanovesicular systems in which a drug is entrapped in a void containing liquid core surrounded by a coat. The objective of the present study was to investigate the potential of polymeric and lipid nanocapsules (LNCs) as innovative carrier systems for miconazole nitrate (MN) topical delivery. Polymeric nanocapsules and LNCs were prepared using emulsification/nanoprecipitation technique where the effect of poly(ε-caprolactone (PCL) and lipid matrix concentrations with respect to MN were assessed.

The resulted nanocapsules were examined for their average particle size, zeta potential, %EE, and in vitro drug release. Optimum formulation in both polymeric and lipidic nanocapsules was further subjected to anti-fungal activity and ex vivo permeation tests. Based on the previous results, nanoencapsulation strategy into polymeric and LNCs created formulations of MN with slow biphasic release, high %EE, and improved stability, representing a good approach for the delivery of MN. PNCs were best fitted to Higuchi’s diffusion while LNCs followed Baker and Lonsdale model in release kinetics.

The encapsulated MN either in PNCs or LNCs showed higher cell viability in WISH amniotic cells in comparison with free MN. PNCs showed less ex vivo permeation. PNCs were accompanied by high stability and more amount drug deposition (32.2 ± 3.52 µg/cm²) than LNCs (12.7 ± 1.52 µg/cm²). The antifungal activity of the PNCs was high 19.07 mm compared to 11.4 mm for LNCs. In conclusion, PNCs may have an advantage over LNCs by offering dual action for both superficial and deep fungal infections.

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Materials: Miconazole nitrate was kindly donated from Sedico Pharmaceutical Company (6th of October City, Egypt). Polycaprolactone was purchased from Sigma-Aldrich Chemical Co. (St. Louis, MO). Propylene glycol dicaprylocaprate (Labrafac^®) was given as a gift by Gattefosse (Saint-Priest, France). Sodium dihydrogen phosphate and disodium hydrogen phosphate were obtained from El-Gomhouria Chemicals Pharmaceutical Company (Cairo, Egypt). Propylene glycol, dichloromethane, and Tween 80 were all pharmaceutical grades and were attained from El-Nasr Chemicals Pharmaceuticals Company (Cairo, Egypt). WISH cell line (normal human epithelial amniotic cells) was obtained at National Cancer Institute (NCI) (Cairo, Egypt). RPMI1640 nutritional media was purchased from Lonza Bioscience (Biological Products Company) (Morristown, NJ).

Article information: Rania S. Abdel-Rashid, Doaa A. Helal, Ahmed Adel Alaa-Eldin & Raghda Abdel-Monem (2022) Polymeric versus lipid nanocapsules for miconazole nitrate enhanced topical delivery: in vitro and ex vivo evaluation, Drug Delivery, 29:1, 294-304, DOI: 10.1080/10717544.2022.2026535