In-Situ Formation of Liposome of Rifampicin: Better Availability for Better Treatment

Praveen   Kumar   Gaur; Shikha      Mishra; V.   B.   Gupta; M.   S.   Rathod; Suresh      Purohit; Bhavin   A.   Savla

doi:10.2174/156720109789941623

Abstract

This study aimed at the preparation and characterization of preformed and in-situ formed liposomes for controlled delivery to the lungs. Two different liposome formulations were prepared and subjected to characterization of physical parameters (vesicle size, appearance, discharge rate, spray pattern and internal pressure) and drug release profile (% cumulative drug release and % drug retained). Formulations were then subjected to accelerated stability studies as per ICH guidelines. It was observed that vesicle size ranged between 2.35 ± 0.23 - 2.41± 0.3 μm and 1.22 ± 0.22- 1.34 ± 0.15 μm respectively for preformed and in-situ formed liposomes. The discharge rate and spray area were in ranges of 110 ± 2.4 -123 ± 2.6 & 115± 2.4 -127±2.3 mg/ actuation & 12.5 ±1.7 -14.1± 2.2 and 13.9 ± 2.1- 14.7± 2.0 cm2 respectively. In-situ liposomes showed better controlled release profile then preformed liposomes as it released 76.5± 2.4 - 58.5 ± 1.8 % drug in 12 hour while retaining 23.5 ± 1.9- 41.5 ± 1.6 % drug whereas preformed liposomes showed cumulative release of 66.5 ± 2.2- 84.5 ± 2.3 % and 15.5 ± 2.4- 33.5± 2.1 % fraction retained. Upon subjection to accelerated conditions for a period of 60 days, preformed liposome completely lost the objective of being controlled release formulation as they showed 92± 2.4 % cumulative release and only 08 ± 1.6 % fraction retained whereas in-situ formulation showed 62 ± 2.3 % cumulative release and 38 ± 2.1 % fraction retained.

Keywords: Tuberculosis, Alveoli, Liposome, Aerosol, Rifampicin, In-situ, Krebs-Henseleit Solution

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