Self-Nanoemulsifying Drug Delivery System (SNEDDS) for Improved Oral Bioavailability of Chlorpromazine: In Vitro and In Vivo Evaluation.

Autor: Baloch J; Sulaiman Bin Abdullah Aba Al-Khail - Centre for Interdisciplinary Research in Basic Science (SA-CIRBS), International Islamic University, Islamabad 44000, Pakistan. jeand_baloch@yahoo.com., Sohail MF; Riphah Institute of Pharmaceutical Sciences (RIPS), Riphah International University, Lahore Campus, Lahore 54770, Pakistan. farmacist@gmail.com.; Department of Pharmacy, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad 45320, Pakistan. farmacist@gmail.com., Sarwar HS; Riphah Institute of Pharmaceutical Sciences (RIPS), Riphah International University, Lahore Campus, Lahore 54770, Pakistan. h_shoaibsarwar@hotmail.com.; Department of Pharmacy, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad 45320, Pakistan. h_shoaibsarwar@hotmail.com., Kiani MH; Department of Pharmacy, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad 45320, Pakistan. marria.h.kyani@gmail.com., Khan GM; Department of Pharmacy, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad 45320, Pakistan. gmkhan@qau.edu.pk., Jahan S; Department of Animal Sciences, Quaid-i- Azam University, Islamabad 45320, Pakistan. sjahan@qau.edu.pk., Rafay M; Department of Forester, Range and Wild life management, College f Agriculture and Environmental Sciences, The Islamia University, Bahawalpur 63100, Pakistan. Rafay@iub.edu.pk., Chaudhry MT; Environmental Analytical Lab, NPSL, Pakistan Council of Scientific and Industrial Research (PCSIR), Islamabad 45710, Pakistan. tausif_chaudhry@yahoo.com., Yasinzai M; Sulaiman Bin Abdullah Aba Al-Khail - Centre for Interdisciplinary Research in Basic Science (SA-CIRBS), International Islamic University, Islamabad 44000, Pakistan. rector@iiu.edu.pk., Shahnaz G; Department of Pharmacy, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad 45320, Pakistan. gshahnaz@qau.edu.pk.
Jazyk: angličtina
Zdroj: Medicina (Kaunas, Lithuania) [Medicina (Kaunas)] 2019 May 24; Vol. 55 (5). Date of Electronic Publication: 2019 May 24.
DOI: 10.3390/medicina55050210
Abstrakt: Background and Objectives: Lipid-based self-nanoemulsifying drug delivery systems (SNEDDS) have resurged the eminence of nanoemulsions by modest adjustments and offer many valuable opportunities in drug delivery. Chlorpromazine, an antipsychotic agent with poor aqueous solubility-with extensive first-pass metabolism-can be a suitable candidate for the development of SNEDDS. The current study was designed to develop triglyceride-based SNEDDS of chlorpromazine to achieve improved solubility, stability, and oral bioavailability. Materials and Methods: Fifteen SNEDDS formulations of each short, medium, and long chain, triglycerides were synthesized and characterized to achieve optimized formulation. The optimized formulation was characterized for several in vitro and in vivo parameters. Results: Particle size, zeta potential, and drug loading of the optimized SNEDDS (LCT 14 ) were found to be 178 ± 16, -21.4, and 85.5%, respectively. Long chain triglyceride (LCT 14 ) showed a 1.5-fold increased elimination half-life (p < 0.01), up to 6-fold increased oral bioavailability, and 1.7-fold decreased plasma clearance rate (p < 0.01) compared to a drug suspension. Conclusion: The findings suggest that SNEDDS based on long-chain triglycerides (LCT 14 ) formulations seem to be a promising alternative for improving the oral bioavailability of chlorpromazine.
Competing Interests: The authors declare no conflict of interest.
Databáze: MEDLINE
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