Abstract
Objective: Nanosuspension is known to enhance the saturation solubility and dissolution velocity of poorly soluble drugs owing to the increased surface area of nanosized particles. Stability of these solubility enhancing systems can be improved by converting them into solidified forms. To simultaneously achieve enhanced dissolution and improved stability, an attempt has been made to increase the dissolution rate of poorly soluble drug tadalafil by formulating immediate release pellets of its nanosuspension.
 Methods: Tadalafil nanosuspensions were prepared using high shear homogenization technique and hydroxypropyl methylcellulose (HPMC) E 15, sodium dodecyl sulphate (SDS) as stabilizers. Prepared nanosuspensions were subjected to the characterization of particle size distribution, zeta potential, drug loading and saturation solubility. Optimized nanosuspension was solidified by preparing immediate release pellets: for improved stability, where tadalafil nanosuspension was used as a binder. Pellets were prepared by extrusion-spheronization technique using κ-carrageenan as a pelletizing aid.
 Results: Prepared immediate release pellets disintegrated within 03 min. In vitro dissolution studies showed 85% drug release within 45 min in pH 1.2 buffer from immediate release pellets containing tadalafil nanosuspension.
 Conclusion: It can be concluded that formulation of nanosuspension of poorly soluble drug and its use as a binder for the preparation of immediate release pellets markedly improved the dissolution rate.
Highlights
One of the major challenges of the pharmaceutical researchers is to develop an enabling formulation which can make poorly water-soluble drugs highly soluble to overcome the low bioavailability problem of the drugs
Particle size data and polydispersity index (PI) result for nanosuspension formulation is shown in table 4
It can be concluded that the formulation of Immediate-release pellets using nanosuspension as a binder can be a novel and feasible option for stabilization as well as solidification of nanosuspensions
Summary
One of the major challenges of the pharmaceutical researchers is to develop an enabling formulation which can make poorly water-soluble drugs highly soluble to overcome the low bioavailability problem of the drugs. Many strategies are used to improve the aqueous solubility of the poorly soluble drugs such as complexation [1], micronisation [2], lipid based formulations, use of cosolvents, solid dispersions [3] etc These techniques often lead to poor solubility, toxicity [4], high production costs [5] and fails at commercial level. Since nanosuspensions suffer from stability problems like aggregation, sedimentation, crystalline transformation, nanosuspension can be solidified by using spray drying method [8], fluid bed drying [9] or by converting into oral thin film [10] formulation These methods may lead to the increased cost of the product. An approach is required that is providing solubility improvement and imparting stability to the formulation during shelf life and which involves simple techniques that can be employed for commercial production
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