Nearly 40% of drugs coming to the market nowadays are having poor solvency related issues and 70% molecules in the discovery pipeline are in effect fundamentally insoluble in water. Nanocrystals is an unmistakable instrument to tackle the issue identified with poor fluid solvency and helps in improving the bioavailability of various drugs as presented in the literature. The particle size reduction came about into the temperamental nanocrystalline system and the phenomenon of ostawald ripening happens. These techniques are preparing to the improvement of nanosized objects, which can play out multiple technological tasks. There are a few couples of noteworthy benefits of nanocrystal formulations, for example, upgrade oral bioavailability, improved dose proportionality, reduced food effects, appropriateness for administration by all routes and probability of sterile filtration because of diminished particle size range. One of the most adequate preferences of nanocrystals is their wide scope of utilization, for example, ophthalmic delivery, oral delivery, transdermal delivery, pulmonary delivery, intravenous delivery and targeted delivery, especially for tumour and brain. The increment in the commercial value of nanocrystals just as the measure of nanocrystal products in the market is picking up more of attention to be utilized as a strategy so as to get commercial advantages. In this paper, a brief and accurate precis of nanosuspension is stated with a specific spotlight on nanosuspension preparation methodologies, benefits and few major applications of nanosuspensions. I In nt te er rn na at ti io on na al l J Jo ou ur rn na al l o of f A Ap pp pl li ie ed d P Ph ha ar rm ma ac ce eu ut ti ic cs s
Objective: To develop two different oral formulations such as 5-fluorouracil (5-FU) tablets and oxaliplatin (OX) microspheres which were further filled into capsules and coated with pH-sensitive polymer (eudragit S-100) for the chronotherapeutic treatment of colon cancer (Fluorouracil: Oxaliplatin regimen) to perform as a substitute for intravenous (IV) route based chronomodulated chemotherapy. Methods: The 5-FU tablet formulation was prepared with alginate and guar gum polymers in varied concentrations using wet granulation technique in two varieties such as granules coated and tablet coated formulations using eudragit RSPO as coating material to achieve controlled drug release. Alongside OX microspheres were formulated using the ionotropic gelation methodology in combination with alginate and chitosan polymers in varying concentrations to accomplish a time-controlled drug release. Prepared formulations were evaluated for pre-compression and post-compression parameters, percentage yield, percentage drug entrapment, Fourier transformed infrared spectroscopy (FT-IR), Differential scanning calorimetry (DSC), Scanning electron microscopy (SEM), In vitro and Ex vivo dissolution studies. Results: Pre-compression and post-compression parameters for 5-FU tablets were satisfied with Indian pharmacopeia specifications. The entrapment efficiency of OX microspheres were increased due to the elevated concentration of polymers up to a certain level as seen in A7M, further greater the concentration of polymer resulted in a decline of entrapment efficiency as seen in A4M and A8M. The optimized formulations A14T and A14M were shown in vitro drug release of 90.36 % by 24 h and 79.63 % by 9 h respectively. Conclusion: The two different oral formulations of 5-FU (Tablets) and OX (Microspheres) were found to be successful in controlled drug release. Therefore they can be efficiently used to control the rate of drug release to the colon in synchronization with the circadian timing system in the belief of improved therapeutic efficacy, tolerability and overall survival rate of cancer patients. Hence it is promised to be a better alternative for intravenous route based chronomodulated chemotherapy.
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