Formulation and Evaluation of Proniosomes of Felodipine

Abstract

Novel drug delivery systems have emerged embracing various routes of administration, oral drug delivery is the most common and preferred method of drug administration. A lipid based drug delivery has become an emerging strategy for improved oral delivery of poorly soluble drugs. Drug encapsulation in the vesicles is one such system which helps to prolong drug duration in systemic circulation and decreases the toxicity by selective uptake. Based on this technique, a number of vesicular drug delivery systems such as liposomes, niosomes and provesicular systems like proliposomes and proniosomes have been developed. The aim of the present investigation was to develop felodipine proniosomes to enhance the solubility. Felodipine loaded proniosomes were prepared by varying ratios of span 60 and cholesterol by solvent evaporation method. Proniosomes were characterized for vesicle size, micromeritics, entrapment efficiency and dissolution behavior. Solid state behavior was evaluated by Differential scanning calorimetry (DSC), Scanning electron microscopy (SEM) and Fourier transform infrared (FTIR) studies. The formulated proniosomes showed improved dissolution characteristics which were assessed from dissolution efficiency, mean dissolution rate data. The transformation of crystalline form of the drug to amorphous and/or molecular state was represented by solid state characterization. FTIR studies showed that absence of interaction between drug and other formulation excipients.

Summary

• Neusilin was selected as suitable solid carrier for formulation of proniosomal felodipine.
• Felodipine loaded proniosomal powders of varying ratios have been prepared successfully by solvent evaporation method.
• Felodipine loaded proniosomal powders upon hydration resulted niosomal tubular structures.
• Micromeritic evaluation showed good to fair flow properties for F1 to F5. Vesicle size of all the formulations found to be within the range of 6 to 14 µm. zeta potential of felodipine loaded proniosomal formulation (F3) was found to be -34.01 mV.
• The entrapment efficiency of all the formulations was found to be between 68% and 72%.
• The formulation containing equimolar ratio of span 60 and cholesterol (F3) showed smaller vesicle size, high zeta potential and entrapment efficiency when compared to other proniosomal formulations.
• The felodipine loaded proniosomal formulation (F3) improved the dissolution of felodipine compared to other formulations. This indicates that enhanced dissolution was also evident from the adsorption of lipid coat on to the solid carrier which increases effective surface area and also due to a possible change in the physical state of the drug from crystalline to amorphous.
• Enhanced dissolution of drug from formulation assessed from parameters such as MDR, IDR and T70% were higher for F3 formulation.
• Solid state characterization revealed transformation of crystalline form of drug to amorphous or molecular state.

DOI: 10.4172/2169-0138.1000154

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