Quality by Design for the Development and Analysis of Enhanced In-Situ Forming Vesicles for the Improvement of the Bioavailability of Fexofenadine HCl In Vitro and In Vivo

Abstract

Drug absorption from the gastrointestinal tract (GIT) is one of the major problems affecting the bioavailability of orally absorbed drugs. This work aims to enhance Fexofenadine HCl oral bioavailability in vivo, the drug used for allergic rhinitis. In this study, novel spray-dried lactose-based enhanced in situ forming vesicles were prepared using different absorption enhancer by the slurry method. Full factorial design was used to obtain an optimized formulation, while central composite design was used to develop economic, environment-friendly analysis method of Fexofenadine HCl in plasma of rabbits. The optimized formulation containing Capryol 90 as absorption enhancer has a mean particle size 202.6 ± 3.9 nm and zeta potential −31.6 ± 0.9 mV. It achieved high entrapment efficiency of the drug 73.7 ± 1.7% and rapid Q3h release reaches 71.5 ± 2.7%. The design-optimized HPLC assay method in rabbit plasma could separate Fexofenadine HCl from endogenous plasma compounds in less than 3.7 min. The pharmacokinetic study and the pharmacological effect of the fexofenadine-loaded optimized formulation showed a significant increase in blood concentration and significantly higher activity against compound 48/80 induced systemic anaphylaxis-like reactions in mice. Therefore, enhanced in situ forming vesicles were effective nanocarriers for the entrapment and delivery of Fexofenadine HCl.

Comprehensive Study of Atorvastatin Nanostructured Lipid Carriers through Multivariate Conceptualization and Optimization

“…The lyophilized AT-NLC formulation did not show the characteristic melting endothermic peak of AT at 160.8 °C, suggesting the presence of AT in the amorphous form within the optimized AT-NLC formulation. The conversion of AT from the ordered crystalline form to the highly energetic disordered amorphous or molecularly dispersed form within the optimized AT-NLC formulation is beneficial for enhancing the AT dissolution rate and hence bioavailability [ 52 ].…”

“…Pharmaceutics 2021, 13, x FOR PEER REVIEW 18 of 24 molecularly dispersed form within the optimized AT-NLC formulation is beneficial for enhancing the AT dissolution rate and hence bioavailability [52].…”

Preparation of Liposomal Formulations for Ocular Delivery of Thymoquinone: In Vitro Evaluation in HCEC-2 e HConEC Cells

“…Consequently, stearic acid, stearin, and linoleic acid, were used to improve the encapsulation efficacy and obtain stable drug delivery systems [28]. In this study Plurol Oleique or polyglycerolodioleate, HLB 3 [29], Maisine or glycerylmonolinoleate, HLB 1 [30], Transcutol P or diethylene glycol monoethyl ether, HLB 4 [31], Capryol 90, propylene glycol monocaprilat, HLB 5 [30], and Lauroglycol 90, glycopropylene monolaureate, HLB 3 [32] were selected to investigate the performance of the developed liposomes. The physical characteristics of 1 mg/mL TQloaded liposomes, prepared with the different liquid lipids, were compared to formulation containg PC plus CH.…”

Liquid and Solid Self-Emulsifying Drug Delivery Systems (SEDDs) as Carriers for the Oral Delivery of Azithromycin: Optimization, In Vitro Characterization and Stability Assessment

“…Medium-chain (C8) TJ opening [33,40,41] Castor Oil -Long-chain (C18) --Octanoic acid (caprylic acid or caprylate) -Medium-chain (C8) TJ opening [42,43] Palm Oil -Long-chain.…”