The in vitro and in vivo study of the nanosuspensions has shown that Co-administration of Curcumin as a p-gp inhibitor with docetaxel may have the potential to increase the anti-breast cancer efficacy of both drugs.
The oral bioavailability of poorly water soluble drug can be improved using nanosuspension. Nanosuspensions are fine dispersion of uniform-sized solid particles in an aqueous vehicle. The present work is aimed at the formulation and evaluation of nanosuspension of felodipine, a poorly water soluble antihypertensive drug. The nanosuspension of felodipine may increase the dissolution rate of drug to improve its oral bioavailability. The nanosuspensions were prepared by nanoprecipitation alone and in combination with ultrasonnication method using ethanol as solvent and water as antisolvent. The prepared nanosuspensions were characterised for particle size, zeta potential, polydispersity index, Scanning electron microscopy (SEM), Differential scanning calorimetry (DSC), X-ray diffraction (XRD) pattern and release behaviour. The effect of variable concentration of drug and stabiliser, ultrasonnication, and solvent to antisolvent ratio on the physical, morphological and dissolution properties of felodipine were studied. The average particle size of felodipine nanoparticles was found to be in the range of 60-330 nm. It was further confirmed by SEM photograph. The particle size varies with increase in concentration of drug and stabiliser. The preparations showed negative zeta potential and polydispersity index in the range of 0.3-0.8. DSC and XRD studies indicated that the crystallinity of precipitated felodipine nanoparticles was markedly lowered than the pure drug. The dissolution of prepared felodipine nanoparticles markedly increased as compared to the original drug. The dissolution profiles of nanosuspension formulation showed up to 79.67 % release in 4 h. It may be concluded that the nanoprecipitation with ultrasonnication have potential to formulate homogenous nanosuspensions with uniform-sized stable nanoparticles of felodipine. The prepared nanosuspension showed enhanced dissolution which may lead to enhanced oral bioavailability of felodipine.
Oral squamous cell carcinoma (OSCC) is one of the common type of cancer in humans. A combinatorial approach has been done by using paclitaxel (PTX), 5-fluorouracil (5-FU) and ascorbic acid (AA) loaded solid lipid nanoparticles (SLN) for its treatment. SLN were made by high-speed homogenization and ultrasonication technique and they were used alone and in combination to check their efficacy against OSCC induced animal model. Pharmacokinetics and biodistribution study of the optimized formulations for PTX, 5-FU and AA loaded SLN was performed. The SLN shows a biphasic nature of drug release both in the in-vitro and in-vivo system. SLN loaded with PTX in combination with SLN loaded with AA shows a greater potency in the treatment of OSCC in-vivo. The Pharmacokinetic and biodistribution studies of SLN depict a better therapeutic efficacy. The combination of PTX and AA loaded SLN can be a novel approach for the treatment of OSCC.
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