Formulation and Evaluation of Novel Hybridized Nanovesicles for Enhancing Buccal Delivery of Ciclopirox Olamine
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Research Article Formulation and Evaluation of Novel Hybridized Nanovesicles for Enhancing Buccal Delivery of Ciclopirox Olamine Mona M. AbouSamra,1 Alaa H. Salama,1,2,5 Ghada E. A. Awad,3 and Soheir S. Mansy4
Received 9 August 2020; accepted 15 September 2020; published online 13 October 2020 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.
KEY WORDS: hybridized vesicles; ciclopirox olamine; buccal delivery; antifungal; oral candidiasis.
INTRODUCTION Candidiasis can be considered the most widespread fungal infection occurring in the mouth, with incidence that varies according to the age and immunity status for the patients. Treatment of buccal candidiasis can be administered either locally or by the systemic route. Local administration is specifically applied to the infected area which provides quite effective treatment of superficial candidiasis (1). A growing interest is focused on developing local antifungal drug delivery systems targeting the oral cavity considering the special physiological characteristics of the mouth (2). Considering the requirement of long-term treatment of 1
Pharmaceutical Technology Department, Pharmaceutical and Drug Industries Research Division, National Research Centre, 33 ElBuhouth Street, Dokki, Cairo, 12622, Egypt. 2 Department of Pharmaceutics, Faculty of Pharmacy, Ahram Canadian University, 6th of October City, Cairo, Egypt. 3 Chemistry of Natural and Microbial product Department, Pharmaceutical and Drug Industries Research Division, National Research Centre, Cairo, 12622, Egypt. 4 Electron Microscopy Research Department, Theodor Bilharz Research Institute,
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