Current Issue : July - September Volume : 2018 Issue Number : 3 Articles : 6 Articles
There are several challenges involved in the development of effective anti-cancer drugs,\nincluding accurate drug delivery without toxic side effects. Possible systemic toxicity and the\nrapid biodegradation of drug carriers are potential risks in the use of carriers for drug-delivery\nformulations. Therefore, the carrier-free drug delivery of an anti-cancer drug is desirable. Herein,\n4-amino-2-benzyl-6-methylpyrimidine (ABMP) was synthesized via a new method using a sodium\ncatalyst, and proved to be effective in inducing breast cancer cell (MDA-MB-231) apoptosis. Moreover,\nthe transparent amorphous state solid of ABMP was demonstrated to have a slow-release property in\nphosphate buffer solution (PBS). Microspheres of ABMP were prepared with diameters in the range\nof 5ââ?¬â??15 Ã?¼m. The slow-release property of the ABMP microspheres indicated their potential use for\ncontrolled-release drug delivery. We believe that microspheres of ABMP have potential as a new kind\nof carrier-free anti-cancer drug delivery system....
The objective of this research work was to enhance solubility and dissolution profile of acyclovir. Nanocrystals were prepared by an anti-solvent precipitation process supplemented by sonication using different stabilizers. The formed nanocrystals were of 376-1085 nm in size. Formulations NC7 and NC8 showed marked improvement in dissolution compared to pure drug, thus greater bioavailability. These nanocrystals were further utilized for the preparation of floating tablet. The nanocrystals based floating tablets were prepared by direct compression technique using different release retardants polymers such as HPMC K100M and carbopol 934P, sodium bicarbonate as gas generating agent in floating sustained release layer. The friability (0.20 to 0.38 %), weight variation (1.17-1.63%) and drug content (96.07 to 98.74 %) of different batch of tablets were found within prescribed limits. The swelling index of tablets composed of carbopol 934P was higher than tablet containing HPMC K100M. The buoyancy lag time was largely dependent on sodium bicarbonate concentration and found to be less than 3 minute for all the optimized tablets (F5, F11 and F13) and was not affected by the polymeric concentrations. The total floating time for different formulations was in the range of 12-30 hours. Release profiles indicated that, increasing the polymer concentration has drastically retarded the release of acyclovir. The optimized tablets F5, F11 and F13 showed 97.47%, 94.57% and 98.83% drug release at the end of 24 hours. Tablets followed non-fickian diffusion controlled first order kinetics. During the stability period selected tablets were found to be stable with respect to physico-chemical and drug release characteristics. Acyclovir pure drug has low solubility and low permeability. The nanocrystal formulation enhances the saturation solubility which increases the dissolution rate and thereby systemic absorption....
In this study, orlistat liposomes were developed and characterized for the physical as well as chemical parameters by ethanol injection method. Formula optimization studies were utilized to investigate the impact of different molar ratios of orlistat drug, soya phosphatidylcholine and cholesterol on physical appearance, pH, density, % drug entrapment efficiency, particle size, polydispersity index and zeta potential. Process optimization studies were also performed to comprehend the effect of variable stirring time, sonication time and centrifugation time on the physical and chemical features. Digital micrographs revealed that the liposomes were in spherical shape. The optimized formulations have about 90.6±0.3% (F30) and 89.0±0.2% (F31) drug entrapment efficiency. Sonication of liposomes was done by probe tip sonicator. Vesicle size, shape and entrapment efficiency were determined by dynamic light scattering, digital microscopy and centrifugation method, respectively. Results showed that high API and cholesterol content resulted in increased entrapment efficiency. Particle size of vesicles was in the nanometers range and uniform in size with no high variability. Zeta potential values of the optimized formulations demonstrated that the liposomes obtained in this study were a dynamic stable system. Effect of alternate method was also seen, thin film hydration method on the physical characteristics as well as the drug entrapment efficiency of orlistat liposomes. Physical appearance was very thin and marginally turbid consistency. No any drug entrapment was observed with the thin film hydration method....
The purpose of the present study was to develop and characterize mesalamine microsphere to target colon for ulcerative colitis. Mesalamine is a drug with low solubility so in order to increase its solubility the solid dispersions of mesalamine were prepared by using kneading method with three different carriers, poly vinyl pyyrolidone (PVP K-30), poly ethylene glycol (PEG 4000) and β-cyclodextrin and evaluated for solubility determination. The solid dispersion (F15) drug: β-cyclodextrin (1:3) was selected for further formulation of microspheres due to its high solubility (4.268±0.031 mg/ml). The microspheres were prepared by using solvent evaporation method. The polymers used were Eudragit L 100 and Eudragit S 100 and glutaraldehyde is used as cross linking agent. The prepared formulations of microspheres were characterized for various parameters like particle size analysis, Scanning electron microscopy, micromeritic properties, percentage yield, drug content, entrapment efficiency, in-vitro release studies and stability studies. The micromeritic properties like angle of repose, Hausner’s ratio and Carr’s index showed good flow properties for all the formulations. The particle size of all formulations was in the range of 203±14 to 437±24 µm. The in-vitro studies revealed that the M6 formulation showed the drug release of 95.12% in a controlled manner up to 14 hrs and the best fit model was Hixson and Crowell which shows that drug release is mainly by dissolution....
Background. Artesunate is one of the most potent, rapidly acting and therapeutically versatile antimalarial drugs. Its efficacy is\nhampered by poor aqueous solubility and stability resulting in low oral bioavailability. Recent efforts to nanoformulate artesunate\nhave shown great potential of improving its dissolution profile and bioavailability.However, no study has yet been done to investigate\nthe intestinal permeability of these nanoformulations, which is a critical determinant of systemic absorption. Objective of the Study.\nThemain aimof the study was to determine the intestinal permeability of artesunate-loaded solid lipid nanoparticles (SLN). Method.\nThemicroemulsion dilution technique was used to fabricate artesunate-loaded solid lipid nanoparticles. In vitro drug release studies\nwere performed at pH 1.2 and 6.8 using the dialysis membrane method.Theeverted gut sac method was used to assess the intestinal\npermeability of the prepared nanoparticles. Results. The average particle size was 1109 nm and the polydispersity index (PDI) was\n0.082. The zeta potential was found to be âË?â??20.7mV. The encapsulation efficiency of the solid lipid nanoparticles obtained was\n51.7%. At both pH 1.2 and 6.8, pure artesunate was rapidly released within the first 30 mins while the SLN showed a biphasic\nrelease pattern with an initial burst release during the first hour followed by a prolonged release over time. The rate of drug release\nincreased with increasing pH. The apparent permeability (...
Vitamin E phosphate (VEP) nucleoside prodrugs are designed to bypass two mechanisms\nof tumor resistance to therapeutic nucleosides: nucleoside transport and kinase downregulation.\nCertain isoforms of vitamin E (VE) have shown activity against solid and hematologic tumors and\nresult in chemosensitization. Because gemcitabine is one of the most common chemotherapeutics for\nthe treatment of cancer, it was used to demonstrate the constructs utility. Four different VE isoforms\nwere conjugated with gemcitabine at the 5 position. Two of these were Ã?´-tocopherol-monophosphate\n(MP) gemcitabine (NUC050) and Ã?´-tocotrienol-MP gemcitabine (NUC052). NUC050 was shown to be\nable to deliver gemcitabine-MP intracellularly by a nucleoside transport independent mechanism.\nIts half-life administered IV in mice was 3.9 h. In a mouse xenograft model of non-small cell lung\ncancer (NSCLC) NCI-H460, NUC050 at a dose of 40 mg/kg IV qwk Ã?â?? 4 resulted in significant\ninhibition to tumor growth on days 11ââ?¬â??31 (p < 0.05) compared to saline control (SC). Median survival\nwas 33 days (NUC050) vs. 25.5 days (SC) ((hazard ratio) HR = 0.24, p = 0.017). Further, NUC050\nsignificantly inhibited tumor growth compared to historic data with gemcitabine at 135 mg/kg IV\nq5d Ã?â?? 3 on days 14ââ?¬â??41 (p < 0.05). NUC052 was administered at a dose of 40 mg/kg IV qwk Ã?â?? 2\nfollowed by 50 mg/kg qwk Ã?â?? 2. NUC052 resulted in inhibition to tumor growth on days 14ââ?¬â??27\n(p < 0.05) and median survival was 34 days (HR = 0.27, p = 0.033). NUC050 and NUC052 have been\nshown to be safe and effective in a mouse xenograft of NSCLC....
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