Abstract：
:Amphotericin B (AmB) liposome formulations are very successful in the treatment of fungal infections and leishmaniasis. But higher cost limits its widespread use among people in developing countries. Therefore, we have developed a modified ethanol-injection method for the preparation of AmB liposomes. Two liposomal formulations were developed with dimyristoyl phosphatidylcholine [F-1a] and soya phosphatidylcholine [F-2a], along with egg phosphatidyl glycerol and cholesterol. AmB was dissolved in acidified dimethyl acetamide and mixed with ethanolic lipid solution and rapidly injected in 5% dextrose to prepare liposomes. Liposomes were characterized on the basis of size (~100 nm), zeta (-43.3 ± 2.8 mV) and percent entrapment efficiency (>95%). The in vitro release study showed an insignificant difference (P ≥ 0.05) for 24-hour release between marketed AmB liposomes (AmBisome) and F-1a and F-2a. Proliposome concentrate, used for the preparation of in situ liposomes, was physically stable for more than 3 months at experimental conditions. Similarly, AmB showed no sign of degradation in reconstituted liposomes stored at 2-8°C for more than 3 months. IC(50) value of Ambisome (0.18 µg/mL) was comparatively similar to F-1a (0.17 µg/mL) and F-2a (0.16 µg/mL) against intramacrophagic amastigotes. Under experimental conditions, a novel modified method for AmB liposomes is a great success and generates interest for development as a platform technology for many therapeutic drug products.
journal_name
J Liposome Resjournal_title
Journal of liposome researchauthors
Singodia D,Verma A,Khare P,Dube A,Mitra K,Mishra PRdoi
10.3109/08982104.2011.584317subject
Has Abstractpub_date
2012-03-01 00:00:00pages
8-17issue
1eissn
0898-2104issn
1532-2394journal_volume
22pub_type
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