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

• Published in: AAPS PharmSciTech Vol. 21; no. 7; p. 283
• Main Authors: AbouSamra, Mona M., Salama, Alaa H., Awad, Ghada E. A., Mansy, Soheir S.
• Format: Journal Article
• Language: English
• Published: Cham Springer International Publishing 13-10-2020
• Subjects: Adhesives; Administration, Buccal; Agar; Animals; Antifungal Agents - administration & dosage; Antifungal Agents - therapeutic use; Biochemistry; Biomedical and Life Sciences; Biomedicine; Biotechnology; Candidiasis, Oral - drug therapy; Candidiasis, Oral - microbiology; Cholesterol - chemistry; Ciclopirox - administration & dosage; Ciclopirox - therapeutic use; Drug Compounding; Drug Liberation; Excipients; Nanoparticles; Particle Size; Pharmacology/Toxicology; Pharmacy; Rabbits; Research Article; Rheology; antifungal; hybridized vesicles; ciclopirox olamine; buccal delivery; oral candidiasis
• ISSN: 1530-9932; 1530-9932
• DOI: 10.1208/s12249-020-01823-9

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.