ABSTRACT

Objective: Oral application of orlistat in the treatment of obesity is limited due to extensive hepatic metabolism, lack of site specific action and short elimination half-life (1-3h). Eudragit coated chitosan orlistat nanoparticles (ECONPs) were designed and evaluated to address the above mentioned limitations. Methods: Chitosan orlistat nanoparticles were designed, optimized by Box-Behnken design. As a challenging enteric coating approach, the optimized formulation was surface coated via simple sonication and lyophilization technique using Eudragit L-100 polymer (a duodenum targeting polymer). Further ECONPs were evaluated for in-vitro characteristics and in-vivo parameters like estimation of body weight, lipid profile viz., total cholesterol (TC), triglycerides (TG), high density lipoproteins (HDL), low density lipoproteins (LDL), very low density lipoproteins (VLDL) along with atherogenic index (AI) and total protein (TP) in obese rats using high fat diet (HFD) model. Results: ECONPs produced better in-vitro characteristics with enhanced in-vitro lipase inhibition and cell viability respectively. ECONPs revealed promising in-vivo potentials with significant reduction (p<0.05) in elevated lipid profiles and body weights along with atherogenic index in obese rats. ECONPs also witnessed increased levels of HDL and TP. Conclusion: ECONPs were found to be promising nanocarriers for targeted delivery and sustained release of orlistat with enhanced in-vivo antiobesity potentials. Keywords: Obesity, orlistat, chitosan, eudragit, nanocarriers
Publication date: 01/07/2023

https://ijbpas.com/pdf/2023/July/MS_IJBPAS_2023_7303.pdf

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https://doi.org/10.31032/IJBPAS/2023/12.7.7303