DEVELOPMENT AND CHARACTERIZATION OF SUSTAINED-RELEASE ARTEMETHERLOADED SOLID LIPID MICROPARTICLES BASED ON MIXED LIPID CORE AND A POLAR HETEROLIPID

DEVELOPMENT AND CHARACTERIZATION OF SUSTAINED-RELEASE ARTEMETHER-LOADED SOLID LIPID MICROPARTICLES BASED ON MIXED LIPID CORE AND A POLAR HETEROLIPID

 

PETRA OBIOMA NNAMANI1 , FRANKLIN CHIMAOBI KENECHUKWU1,* , JUDITH CHIAMAKA OMEJE1 , LYDIA ONYINYECHI NWACHUKWU2 , AGATHA ADAORA UGWU3 , FRANCIS IFEANYI ANAZODO4 , CHINEKWU SHERRIDAN NWAGWU1 , ADEOLA TAWAKALITU KOLA-MUSTAPHA5 , NICHOLAS CHINEDU OBITTE2 , ANTHONY AMAECHI ATTAMA1
  1. Drug Delivery and Nanomedicines Research Unit, Department of Pharmaceutics, Faculty of Pharmaceutical

           Sciences, University of Nigeria, Nsukka 410001, Enugu State, Nigeria.

  1. Department of Pharmaceutical Technology and Industrial Pharmacy, University of Nigeria, Nsulkka 410001, Enugu State, Nigeria.
  1. Department of Pharmaceutics and Pharmaceutical Technology, Enugu State University of Science and Technology, Agbani, Enugu State, Nigeria.
  1. Department of Pharmaceutical Microbiology and Biotechnology, Madonna University, Elele, Rivers State, Nigeria.
  2. Department of Pharmaceutics and Industrial Pharmacy, University of Ilorin, Ilorin, Nigeria.

Afr. J Pharm Res Dev; Volume 14(1): 001-017 ; Jan – June 2022

ABSTRACT

The objective of this study was to formulate and evaluate artemether-loaded solid lipid microparticles SLMs from

templated captex 300® and Capra hircus (goat fat) homolipid for sustained delivery in the treatment of malaria.

Various ratios of captex 300®, goat fat and Phospholipon® 90G were used to prepare the templated lipid matrices

and characterized by differential scanning calorimetry (DSC). The templated lipid matrices were employed to

formulate SLMs containing various concentrations (1.0, 3.0 and 5.0 %w/v) of artemether by melt-emulsification

technique. Physicochemical characterizations were performed on the SLMs with respect to mean particle size,

morphology, encapsulation efficiency, compatibility, time-dependent pH stability and drug release in phosphate

buffered saline (PBS, pH 7.4) compared with artemether injection (control). The DSC results showed that the

formulated lipid matrices were suitable for the development of the SLMs. Stable spherical artemether-loaded SLMs

with encapsulation efficiency and mean particle size that ranged from 20.49 ± 1.15 % to 87.02 ± 3.13 % and 1.60

± 0.05 µm to 21.30 ± 0.50 µm, respectively, were developed. Among the formulations, SLMs based on Captex

300® and goat fat (1:1) at 1.0 and 3.0% artemether concentrations (batches A1 and A2) as well as SLMs based on

Captex 300® and goat fat at (2:1) at 1.0% artemether concentration (batch C1) gave significantly (p<0.05) greater

in vitro drug release in PBS than artemether injection. This study has shown that artemether-loaded SLMs based

on Captex 300® and goat fat templated with Phospholipon® 90G could be employed as an alternative sustained

release formulation than artemether injection for enhanced malaria treatment.

 

Email of correspondence: frankline.kenechukwu@unn.edu.ng;

KEYWORDS: Artemether-loaded solid lipid microparticles (SLMs); sustained release; Capra hircus (goat fat); captex 300®; Phospholipon® 90G.