Buspirone Hydrochloride Loaded In Situ Nanovesicular Gel as an Anxiolytic Nasal Drug Delivery System: In Vitro and Anima
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Research Article Buspirone Hydrochloride Loaded In Situ Nanovesicular Gel as an Anxiolytic Nasal Drug Delivery System: In Vitro and Animal Studies Dina M. Abdelnabi,1 Marwa H. Abdallah,1,2,3 and Hanaa A. Elghamry1
Received 6 June 2018; accepted 8 October 2018 Abstract.
Nasal nanovesicular gels of buspirone hydrochloride (BH) were prepared and characterized aiming for sustained delivery and enhancing bioavailability. Buspirone hydrochloride has low bioavailability of about 4% after oral administration due to first pass metabolism. Buspirone hydrochloride nanovesicles were formulated by thin film hydration method (TFH). The selected nanovesicular formulation was incorporated into two types of in situ gels (pH-induced and thermoreversible) using carbopol 974P and poloxamer 407 (P407), respectively, together with different mucoadhesive polymers. The in situ gels were examined for pH, gelling capability, viscosity, content uniformity, mucoadhesiveness, and in vitro drug release. The ex vivo permeation performance of the in situ gel formulations that showed the most sustained release was also assessed. The in vivo study was done by the determination of BH blood level in albino rabbits after nasal administration. Results revealed that nanovesicles prepared using Span 60 and cholesterol in a ratio of 80:20 showed the highest EE% (70.57 ± 1.00%). The ex vivo permeation data confirmed higher permeability figures for carbopol formulation in comparison to poloxamer formulations. The in vivo study data showed an increase of 3.26 times in BH bioavailability when formulated into the carbopol nanovesicular in situ gel relative to control (nasal drug solution).
KEY WORDS: buspirone hydrochloride; nanovesicles; spans; cholesterol; poloxamer; carbopol.
INTRODUCTION Nanovesicles are drug carriers analogous to phospholipid vesicles (liposomes) and can serve as useful drug carriers (1) which offer advantages such as chemical and physiochemical stability. The inclusion of drugs into nanovesicles can lower drug toxicity, boom drug absorption, and retard the clearance of the drug from the blood stream due to tardy drug release (2). Buspirone hydrochloride (BH) is a water-soluble drug that is used to treat generalized anxiety disorder through its serotonin agonist activity. In addition, conditions such as autism and pervasive development disorder in children may be related to alterations in brain serotonin synthesis, suggesting that BH might have value in such treatment (3). Recent studies have shown that nasal route can be valuable for systemic delivery of low bioavailability drugs (4) as well as drugs that undergo extensive first pass
1
Department of Pharmaceutics, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt. 2 Department of Pharmaceutics, College of Pharmacy, Hail University, Hail, Kingdom of Saudi Arabia. 3 To whom correspondence should be addressed. (e–mail: [email protected])
metabolism. This route also has an extra advantage of direct brain targeting via the olfactory route (5). Generally, conventional nasal
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