Formulation and characterization of artemether-loaded sodium alginate microcapsules

Anthony A Attama,Godswill C Onunkwo,John-Dike N Ogbonna,Paul A Akpa,Obialunamma C Metu,Ifeanyi T Nzekwe,Petra O Nnamani,Adaeze C Echezona,Simeon U Onoja

doi:10.4314/tjpr.v19i7.1

Abstract

Purpose: To increase the solubility of artemether (ART) in Transcutol® HP through microencapsulation in sodium alginate polymer to achieve sustained in vivo release.Method: Graded concentrations of ART (0.00, 0.25, 0.50, 0.75, and 1.00 g) microcapsules were produced using Tween® 80 by the cold homogenization method at 24 x 1000 rpm for 15 min. Characterization based on yield, encapsulation efficiency (EE), particle size, pH stability, differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR) and in vivo release using Peter’s four-day suppressive protocol in Wistar mice infected with Plasmodium berghei, were determined.Results: The results obtained indicate that 0.5 g ART-loaded microcapsules (AMC) showed the highest yield of 96.85 %. The EE of 88.3 % corresponded to 0.75 g ART-loaded microcapsules. DSC results revealed that there was a significant reduction in enthalpy in all the formulations compared to the crystalline drug, but no strong bond interaction occurred except for the blank microcapsules. The AMC1.0 showed high dose-dependent plasmodial growth inhibition of 88.75 % while AMC0.25 had the least (68.13 %).Conclusion: The artemether microcapsules showed sustained release characteristics for oral delivery of artemether and therefore may reduce some of the adverse effects associated with high dose artemether therapy in conventional oral tablets. Keywords: Malaria, Artemether, Transcutol® HP, Sustained-release, RBC count, Antiplasmodial activity

Highlights

Malaria is a poverty-related disease and its mortality burden is high in Africa [1].Interventions geared towards malaria reduction has significantly reduced the morbidity and mortality rates greatly
The country accounts for 25 % out of the 93 % of global malaria deaths in 2018 that was concentrated in 17 countries in the WHO African Region and India
The results of the pH test carried out post formulation of microcapsule dispersions (1 week, 1 and 3 months) of the drug-loaded microcapsules and unloaded microcapsule showed mean pH range of 8.44 ± 0.22 to 9.62 ± 0.11, 8.71 ± 0.96 to 9.22 ± 1.89, 8.58 ± 0.05 to 9.28 ± 0.09, 8.72 ± 0.02 to 9.82 ± 0.07, and 8.75 ± 0.12 to 9.62 ± 0.07 relative to AMC0.25, AMC0.5, AMC0.75, AMC1.0 and ART-loaded microcapsules (AMC) unloaded, respectively

Summary

Introduction

Malaria is a poverty-related disease and its mortality burden is high in Africa [1]. Interventions geared towards malaria reduction has significantly reduced the morbidity and mortality rates greatly. Malaria is still the major cause of mortality and morbidity. Nigeria is one of the ten highest burden countries in Africa reported to have increased cases of malaria. The country accounts for 25 % out of the 93 % of global malaria deaths in 2018 that was concentrated in 17 countries in the WHO African Region and India. Children under 5 years are the most susceptible group disturbed by malaria and account for 65 % of all the global malaria demises. The consequence of malaria is felt by the poor population of third world countries especially in Africa where the people cannot afford the expensive drugs. Monotherapy has given way to artemisinin-combination therapies (ACTs)

Results

Discussion

Conclusion