The objective of this work was to study dissolution enhancement efficiency and solid dispersion formation ability of hydrophilic swellable polymers such as sodium carboxymethyl cellulose (Na-CMC), sodium starch glycolate (SSG), pregelatinized starch (PGS), and hydroxypropylmethyl cellulose (HPMC) with carbamazepine using 3 2 full factorial design for each of the polymers. Solid dispersions of carbamazepine were prepared using solvent evaporation method with around 70% solvent recovery. The independent variables were the amount of polymer and organic solvent. The dependent variables assessed were percentage drug dissolved at various time points and dispersion efficiency (ie, in terms of particle size of solid dispersion). Solid dispersions were evaluated for percentage drug dissolved, wettability, differential scanning calorimetry, scanning electron microscopy, and angle of repose. Multiple linear regression of results obtained led to equations, which generated contour plots to relate the dependent variables. Similarity factor and mean dissolution time were used to compare dissolution patterns obtained in distilled water and simulated gastric fluid United States Pharmacopeia (USP) XXVI of pH 1.2. Maximum drug dissolution was obtained with polymer order Na-CMC9SSG9PGS9HPMC. Particle size of drug was reduced~10-15, 3-5, 5-7, and 10-25 times in Na-CMC, SSG, PGS, and HPMC solid dispersions, respectively; whereas wettability of solid dispersions was found in the order of Na-CMC9HPMC9PGS9SSG. Angle of repose was found to be in the range of 29°to 35°for all solid dispersions, which shows good flowability characteristics. HPMC showed increase in drug dissolution up to an optimized level; however, further increase in its concentration decreased drug dissolution.

The objective of the present investigation was to reduce the bitterness with improved dissolution, in acidic medium (pH 1.2), of mefloquine hydrochloride (MFL). Microparticles were prepared by coacervation method using Eudragit E (EE) as polymer and sodium hydroxide as precipitant. A 3(2) full factorial design was used for optimization wherein the drug concentration (A) and polymer concentration (B) were selected as independent variables and the bitterness score, particle size and dissolution at various pH were selected as the dependent variables. The desirability function approach has been employed in order to find the best compromise between the different experimental responses. The model is further cross validated for bias. The optimized microparticles were characterized by FT-IR, DSC, XRPD and SEM. Bitterness score was evaluated by human gustatory sensation test. Multiple linear regression analysis revealed that the reduced bitterness of MFL can be obtained by controlling the dissolution of microparticles at pH 6.8 and increasing the EE concentration. The increase in polymer concentration leads to reduction in dissolution of microparticles at pH > 5 due to its insolubility. However the dissolution studies at pH 1.2 demonstrated enhanced dissolution of MFL from microparticles might be due to the high porosity of the microparticles, hydrophilic nature of the EE, and improved wettability, provided by the dissolved EE. The bitterness score of microparticles was decreased to zero compared to 3+ of pure ARM. In conclusion the bitterness of MFL was reduced with improved dissolution at acidic pH.

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In the present work effect of chitosan on microcrystal formulation for dissolution enhancement of oxcarbazepine using controlled crystallization technique coupled with spray drying was explored. The work was extended for exploration of simplified approach for stable particle size reduction. The study was performed with an experimental design approach i. e. a fractional factorial design of resolution 5 (with all 2 factor interaction) for the screening of predefined independent variables drug concentration, chitosan concentration, feed rate, inlet temperature and percent aspiration for spray drying. Whereas percent drug dissolved, wettability time, flowability in terms of angle of repose and particle size were designated as response variables. Resultant models were analyzed using multiple linear regression analysis, which generated equation to plot response surface curves along with desirability function. Results showed that chitosan concentration had significant effect on dissolution enhancement of oxcarbazepine at a level of 2% w/v. Increase in drug concentration showed decreased dissolution rate however on particle size it did not show statistically significant effect. Topographical characterization was carried out by SEM which showed that feed rate, percent aspiration and inlet temperature had significant effect on particle morphology. For deriving optimized formulation results were analyzed using desirability function for the maximum percent drug dissolved and least drug polymer matrix particle size. DSC studies showed that drug was molecularly associated with chitosan matrix or particles.

Nanomedicine is focused on the development of submicrometer carriers designed for improving the biodistribution of systemically administered drugs. Nanoparticles have been exploited for immunoassays, immunohistochemistry, cancer diagnostics, bioseparation of specific cell populations, and cellular imaging. Public awareness on the use of these novel therapeutic approaches is increasing due to the exponential boom of nanotechnologies in the latest years. With respect to cancer therapy, several tumour-targeted nanomedicines have been evaluated over the years, and there is a clear evidence for substantial improvement of the therapeutic index of antineoplastics. The present review addresses the most relevant targeting strategies, discussing the major public awareness, therapeutic advances and future directions in the development of tumour-targeted nanomedicines.