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ACTIVE ENTRAPMENT OF AMPHOTERICIN B
LIPOSOMES USING pH, SURFACE CHARGE
SURFACTANT, AND CO-SOLVENT
MISS KUNNATEE CHAIYAWAT
MISS NUTCHA SUPPATRANON
A SPECIAL PROJECT SUBMITTED IN PARTIAL FULFILMENT
OF THE REQUIREMENT FOR
THE BACHELOR DEGREE OF SCIENCE IN PHARMACY
FACULTY OF PHARMACY
MAHIDOL UNIVERSITY
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Abstract
Active entrapment of amphotericin B liposomes using pH, surface
charge, surfactant, and co-solvent.
Kunnatee Chaiyawat, Nutcha Suppatranon
Project advisor Narong Sarisuta
Department of Manufacturing Pharmacy, Faculty of Pharmacy, Mahidol University
Key word : amphotericin B liposomes, pH, stearylamine, Span 20, dimethylsulfoxide
The objective of this project was to develop the formulations of amphotericin B
liposomes by chloroform film method with high percentage loading and entrapment
efficiency, which was carried out by adjusting the amount of drug added (2-10 %w/w)
and pH (4.0 and 7.2), introducing surface charge (stearylamine), using surfactant (Span
20) and co-solvent (dimethylsulfoxide) in the system. From the studies of
physicochemical properties of amphotericin B liposomes by determining percentage
loading, entrapment efficiency, and size of liposomes, it was found that the percentage
loading of the drug increased with the increasing amount of the drug added in to the
formulation. The factor that had an obvioiusly effect to the percentage loading of the
drug was surfactant (Span 20) and co-solvent (dimethylsufoxide). The best formula
having maximum percentage loading was the one with the use of co-solvent
(dimethylsulfoxide) but without surfactant (Span 20). The formula with maximum
entrapment efficiency was the one with 4 %w/w of drug added so that the drug could be
completely dissolved. The factor that had an obvioius effect on the entrapment
efficiency was surfactant (Span 20) and the best formula having maximum percentage
loading was the one without surfactant (Span 20). The sizes of all liposomal formulations
were found to vary from 1,000 - 30,000 nm. However, in the production of liposomes,
they were usually subject to uniform size reduction before use.