Solubility Enhancement Essay

814 Words 4 Pages
The development of new drug discovery technologies like high throughput screening, combinatorial chemistry, etc. has led to the discovery of a large number drugs that are poorly water soluble.(1,2) Approximately 40% of the NCEs are poorly water soluble and has poor bioavailability.(3) The successful clinical use of these molecules requires the application of solubility enhancement based formulation approaches.
Among the various solubility enhancement technique like use of cosolvents, emulsification, preparation of solid dispersions, micronization, complexation, cocrystalisation, liposomes, etc., nanonization technology has gained much popularity. (4-18) Drug nanocrystals possesses several advantages like enhanced solubility, dissolution rate
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Stabilizers; PVP K30, PVA, Pluronic® F-68 and PEG 4000 was purchased from HiMedia. HPMC was purchased from Colorcon. Pluronic® F-127 was purchased from Sigma Aldrich. Mannitol was from Spectrochem, Mumbai. All the solvents; methanol, acetone and DCM was purchased from Fischer Scientific.

Preparation of nanosuspension:
Nanosuspension was prepared by antisolvent precipitation method. The effect of various factors on the particle size, pdi and zeta potential of the formulation was carried out by single factor experiment including stabilizers (PVP K30, HPMC, F68, F127, PEG4000), organic phase species (acetone, methanol, DCM), volume of organic solvent and speed of stirring. Drug dissolved in the organic solvent was added drop wise from a syringe to an aqueous solution of stabilizer kept under magnetic stirring at a rate of one drop per three second.
Drying of nanosuspension using electrospray technique:
The electrospraying was carried out with Epsin Nano device. The nanosuspension was added to 1% PVA solution. The conditions for electrospraying included a voltage of 25kV, feed rate of 2ml/hr and a cabin temperature of 45°C. A distance of 10cm was maintained between the needle and the

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