Response Surface Methodology for Optimization of Buspirone Hydrochloride-Loaded In Situ Gel for Pediatric Anxiety

Abstract

The purpose of the current investigation was to formulate, assess, and optimize oral in situ gels of buspirone hydrochloride (BH) with the specific end goal of expanding the time the medication spends in the stomach, thereby ensuring an extended medication discharge. This would allow the use of a once-a-day dose of liquid BH formulations, which is ideal for the treatment of pediatric anxiety. In situ gels loaded with BH were prepared using various concentrations of sodium alginate (Na alg.), calcium chloride (CaCl2), and hydroxypropyl methylcellulose (HPMC K15M). The in situ gels exhibited the desired consistency, drug distribution, pH, ability to form gel, and prolonged drug release in vitro. The (33) full factorial design was utilized for the revealing of the ideal figures for the selected independent variables, Na alg. (X1), HPMC (X2), and CaCl2 (X3) based on measurements of the viscosity (Y1) and percentage drug release after 6 h (Y2). A pharmacokinetic study of the optimum formulation on rabbits was also performed. The formulation containing 2% of Na alg., 0.9% of HPMC-K15M, and 0.1125% of CaCl2 was selected as the ideal formulation, which gave the theoretical values of 269.2 cP and 44.9% for viscosity and percentage of drug released after 6 h, respectively. The pharmacokinetic study showed that the selected oral Na alg. in situ gel formulation displayed a prolonged release effect compared to BH solution and the marketed tablet (Buspar®), which was confirmed by the low Cmax and high Tmax values. The optimum oral Na alg. in situ gel showed a 1.5-fold increment in bioavailability compared with the drug solution.

Ginger Extract-Loaded Sesame Oil-Based Niosomal Emulgel: Quality by Design to Ameliorate Anti-Inflammatory Activity

“…Central composite (CC) design was used to conduct the analysis of variance for the investigated dependent responses, and ANOVA was used to acquire specific parameters such as p -value, F-value, and model F-value [ 21 ]. The quadratic model had the best fit for all responses comparing to all other models.…”

Formulation and Evaluation of Polysaccharide Microparticles for the Controlled Release of Propranolol Hydrochloride

“…Sodium alginate is widely used for the encapsulation of active substances because it has the ability to form a gel structure, such as the “egg-box”, as a result of cross-linking with calcium ions (ionotropic gelation process) [ 14 ]. In previous studies, sodium alginate was combined with different polymers, such as hydroxypropyl methylcellulose, polyvinyl alcohol, and gelatin, to formulate dosage forms for pediatric use [ 15 , 16 ].…”

Tailoring Risperidone-Loaded Glycethosomal In Situ Gels Using Box–Behnken Design for Treatment of Schizophrenia-Induced Rats via Intranasal Route

“…Furthermore, the extended duration of their presence at the site of application can lead to an augmentation in the drug penetration across the nasal mucosa, hence enhancing its bioavailability [12]. On another side, utilizing mixtures of gelling agents is interestingly followed to acquire more benefits to the in situ gel products after observing their behavior [13,14]. These mixtures can offer new points of view about the thermo-sensitive delivery systems, for example, positively affecting their gel strength and elasticity, improving their physical properties, controlling the drug release, and facilitating the dosage administration [15].…”