Mixed micelles for bioavailability enhancement of nelfinavir mesylate: In vitro characterisation and In vivo pharmacokinetic study

ABSTRACT

The present investigation deals with the fabrication of Nelfinavir mesylate loaded mixed micelles (NFM-MM) to enhance its oral bioavailability. NFM is a Human Immunodeficiency Virus-1 protease inhibitor having poor oral bioavailability and pH-dependant aqueous solubility leading to frequent dosing. Mixed micelles of Pluronic F127 and D-α-tocopherol polyethylene glycol 1000 succinate were prepared by thin film hydration technique. Results of in vitro characterisation showed that NFM-MM exhibited particle size 104.1 nm, polydispersity index (PDI) 0.127, zeta potential −10.6 mV, % entrapment efficiency 99.76 ± 1.20 and % drug loading 19.51 ± 1.02. DSC and P-XRD studies confirmed that NFM was encapsulated inside the mixed micelles. The in vitro release studies revealed that NFM-MM showed sustained release for upto four days. These mixed micelles were spherical or elliptical in shape as revealed by TEM study. On oral administration of NFM-MM; the relative bioavailability was enhanced about 1.94 fold as compared to NFM suspension. Thus, it can be concluded that PF127/TPGS mixed micelles can be used as a promising delivery system for NFM with increased bioavailability and sustained drug release.

Graphical Abstract

KEYWORDS:

• Nelfinavir mesylate
• Pluronic F127
• TPGS
• mixed micelles
• bioavailability enhancement

Disclosure statement

The authors report no conflicts of interest in this work.