TY - JOUR
T1 - Assessment of formulated amodiaquine microparticles in Leishmania donovani infected rats
AU - Nettey, Henry
AU - Allotey-Babington, Grace Lovia
AU - Somuah, Isaac
AU - Banga, N’guessan Benoit
AU - Afrane, Barima
AU - Amponsah, Seth Kwabena
AU - Annor, Henrietta
AU - Darko, Henry
AU - Hanson, Kwame
AU - Aidoo, Anoa
AU - Broni, Marisa Nyarkoa
AU - Sasu, Clement
AU - Nyarko, Alexander
N1 - Publisher Copyright:
© 2017 Informa UK Limited, trading as Taylor & Francis Group.
PY - 2017/1/2
Y1 - 2017/1/2
N2 - The aim of this study was to formulate, characterise and evaluate the activity of amodiaquine microparticles against Leishmania donovani. Microparticles were formulated by encapsulating the drug in bovine serum albumin using the spray-dryer method. The microparticles were evaluated for size, zeta potential, drug content, encapsulation efficiency and in vitro release profile. The size range of the microparticles formulated was between 1.9 and 10 μm with an average zeta potential of −25.5 mV. Of the expected 20% drug loading, an average of 18.27% was obtained giving an encapsulation efficiency of 91.35%. Pharmacokinetic profile of amodiaquine improved with microencapsulation of the drug with Cmax, AUC0→48 and t1//2 all significantly higher than amodiaquine solution. Amodiaquine microparticles showed an overall higher bioavailability and hence were more effective in eliminating intra-tissue parasites than the drug solution. It would therefore be expected that the formulated microparticles will be more effective in treating visceral leishmaniasis.
AB - The aim of this study was to formulate, characterise and evaluate the activity of amodiaquine microparticles against Leishmania donovani. Microparticles were formulated by encapsulating the drug in bovine serum albumin using the spray-dryer method. The microparticles were evaluated for size, zeta potential, drug content, encapsulation efficiency and in vitro release profile. The size range of the microparticles formulated was between 1.9 and 10 μm with an average zeta potential of −25.5 mV. Of the expected 20% drug loading, an average of 18.27% was obtained giving an encapsulation efficiency of 91.35%. Pharmacokinetic profile of amodiaquine improved with microencapsulation of the drug with Cmax, AUC0→48 and t1//2 all significantly higher than amodiaquine solution. Amodiaquine microparticles showed an overall higher bioavailability and hence were more effective in eliminating intra-tissue parasites than the drug solution. It would therefore be expected that the formulated microparticles will be more effective in treating visceral leishmaniasis.
KW - Amodiaquine; Leishmania donovani
KW - albumin
KW - microparticles
KW - pharmacokinetics
UR - http://www.scopus.com/inward/record.url?scp=85010671916&partnerID=8YFLogxK
U2 - 10.1080/02652048.2017.1280094
DO - 10.1080/02652048.2017.1280094
M3 - Article
C2 - 28067090
AN - SCOPUS:85010671916
SN - 0265-2048
VL - 34
SP - 21
EP - 28
JO - Journal of Microencapsulation
JF - Journal of Microencapsulation
IS - 1
ER -