Abstract
Objective: The objective of the present study was to formulate and evaluate liposomes loaded with isoniazid.Methods: Liposome of isoniazid was made by thin layer film hydration method. L-α-phosphatidylcholine and cholesterol were used to make multiamellar vesicles. Six batches of liposomes were prepared based on the different weight ratio of L-α-phosphatidylcholine and cholesterol. Differential scanning calorimetry (DSC) study conducted to study in any incompatibility.Results: The prepared liposomes were evaluated by particle size analysis, entrapment efficiency, release study and stability study. Particle sizes were determined from the scanning electron microscopy (SEM) photographs. When particle frequencies were plotted against particle diameter in the histogram, it showed that F1 batch had a skewed distribution towards smaller liposomes while F6 shows a proper bell-shaped curve with a mean at 225 mm. The percentage entrapment efficiency was found to be 8.99 ± 0.15 to 4.19 ± 0.12 % respectively. From the release profile, it was seen that F1 batch was fastest and F6 was slowest to release the drug. The satisfactory batch F1 was packed in Eppendorf tube and stored at 4 °C temperature for one month. At the end of one month, the samples were analyzed for their physical properties, drug entrapment and in vitro release profile. The percentage release was found to be 96.5 ± 3.2 after 4 h.Conclusion: The F1 batch showed most promising results compared to other. No significant change was found during one month’s stability study of final batch (F1).
Highlights
Liposome has become an essential therapeutic tool most notably in drug delivery and targeting
L-α-phosphatidylcholine, cholesterol were purchased from yarrow Chem., Mumbai
The melting point of the pure Isoniazid was found from the peak of Differential scanning calorimetry (DSC) thermogram at 172.81 °C
Summary
Liposome has become an essential therapeutic tool most notably in drug delivery and targeting. The hydrated lipid sheets get detached during agitation and self-close to form large, multiamellar vesicles (MLVs), which prevent interaction of water with the hydrocarbon core of the bilayer at the edges. Once these MLVs are formed, a change in vesicle shape and morphology may require energy input in the form of sonic energy and/or mechanical energy. The former produce small unilamellar vesicles (SUVs) while the latter usually produces large unilamellar vesicles. Liposomal drug delivery system is very useful for delivery of anticancer, antifungal, antibacterial, antiparasites, ocular and antiviral drugs [2,3,4]
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