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Formulation and Evaluation of Novel Hybridized Nanovesicles for Enhancing Buccal Delivery of Ciclopirox Olamine

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Abstract

Ciclopirox olamine (CPO) is a topical wide-spectrum antimycotic agent that possesses antifungal, antibacterial and anti-inflammatory activities. Loading CPO into a hybridized vesicular system is expected to enhance its buccal permeation and hence, therapeutic activity, whereas the frequent administration and side effects are reduced. Vesicular systems with high penetration ability were prepared based on cholesterol, Lipoid S45 or Phospholipon 90H, with span 60 while incorporating a penetration enhancer (Labrafac or labrasol) followed by full assessment of their size, entrapment efficiency, and drug release profiles. The optimum formulation, composed of Lipoid S45 and Labrafac, possessed the smallest vesicle size (346.1 nm), highest entrapment efficiency (94.4%), and sustained CPO release pattern, and was characterized for its morphology and thermal properties. This powerful mixture of the penetration enhancers (Lipoid S45 and Labrafac) in the designed hybridized vesicles was thoroughly investigated for their characteristics after being incorporated in bioadhesive gel. Moreover, enhanced antifungal activity was demonstrated either upon testing the designed formulation on agar plates or in vivo upon treating infected rabbits with the proposed formulation. Results suggest that the presented bioadhesive gel incorporating the CPO-loaded vesicles can be a promising delivery system that can offer a prolonged localized antifungal treatment with enhanced therapeutic effect.

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Funding

This study received financial support from the National Research Centre through a grant (No: 11010301).

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Authors and Affiliations

  1. Pharmaceutical Technology Department, Pharmaceutical and Drug Industries Research Division, National Research Centre, 33 El-Buhouth Street, Dokki, Cairo, 12622, Egypt

    Mona M. AbouSamra & Alaa H. Salama

  2. Department of Pharmaceutics, Faculty of Pharmacy, Ahram Canadian University, 6th of October City, Cairo, Egypt

    Alaa H. Salama

  3. Chemistry of Natural and Microbial product Department, Pharmaceutical and Drug Industries Research Division, National Research Centre, Cairo, 12622, Egypt

    Ghada E. A. Awad

  4. Electron Microscopy Research Department, Theodor Bilharz Research Institute, Cairo, Egypt

    Soheir S. Mansy

Authors
  1. Mona M. AbouSamra
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  2. Alaa H. Salama
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  3. Ghada E. A. Awad
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  4. Soheir S. Mansy
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Correspondence to Alaa H. Salama.

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AbouSamra, M.M., Salama, A.H., Awad, G.E.A. et al. Formulation and Evaluation of Novel Hybridized Nanovesicles for Enhancing Buccal Delivery of Ciclopirox Olamine. AAPS PharmSciTech 21, 283 (2020). https://doi.org/10.1208/s12249-020-01823-9

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  • DOI: https://doi.org/10.1208/s12249-020-01823-9

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