Sivaram Nallamolu¹*, Vijaya Ratna Jayanti², Mallikarjun Chitneni³ and Prashant Kesharwani¹

¹School of Pharmacy, Department of Pharmaceutical Technology, International Medical University, Kuala Lumpur, Malaysia
²Andhra University College of Pharmaceutical Sciences, Andhra University, Visakhapatnam, AP, India
³Jurox Pty Limited, Rutherford New South Wales, Australia

*Corresponding Author: Sivaram Nallamolu, School of Pharmacy, Department of Pharmaceutical Technology, International Medical University, Kuala Lumpur, Malaysia.

Received: December 27, 2017; Published: February 02, 2018

Citation: Sivaram Nallamolu., et al. “Solubility Enhancement of Poorly Water-Soluble Drug Aprepitant for Oral Delivery by Self-Micro Emulsifying Drug Delivery System”. Acta Scientific Pharmaceutical Sciences 2.3 (2018).

Abstract

  The objective of the present study was to develop self microemulsifying drug delivery system (SMEDDS) for improving the delivery of a BCS class IV antiemetic drug, aprepitant (APT). The in vitro self-emulsification properties, droplet size analysis, drug content, polydispersity index, zeta potential etc. of these formulations upon their addition to water under mild agitation conditions were studied. The solubility of APT was found to be high in Capryol90 (12.53 ± 0.35); Labrasol (13.30 ± 0.23); Transcutol HP (49.15 ± 0.28) mg/ml. The range of mean droplet size was 13.97 ± 0.72 nm to 124.90 ± 0.20 nm while the polydispersibility values were in the range of 0.169 to 0.604 with a zeta potential of -41.1 mV. More than 90% of the drug released within 30 minutes when compared with pure drug release of 13% in 30 minutes. The SMEDDS formulations followed first order kinetics. The APT formulations were proved to be robust, stable to pH, and thermodynamically stable and formed clear transparent micro emulsions in few seconds. Thus, the study confirmed that the Aprepitant SMEDDS formulation can be used as a possible alternative to traditional oral formulations to improve its bioavailability.

Keywords: Aprepitant; SMEDDS; Ternary Phase Diagram; Micro Emulsion; Solubility

Copyright: © 2018 Sivaram Nallamolu., et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.