Current Issue : October - December Volume : 2017 Issue Number : 4 Articles : 5 Articles
Glucocorticoids are widely prescribed in treatment of rheumatoid arthritis, asthma, systemic\nlupus erythematosus, lymphoid neoplasia, skin and eye inflammations. However, well-documented\nadverse effects offset their therapeutic advantages. In this work, novel nano-hydrogels for the\nsustained delivery of dexamethasone were designed to increase both bioavailability and duration of\nthe administered drug and reducing the therapeutic dose. Hydrogels are soft materials consisting\nof water-swollen cross-linked polymers to which the insertion of cyclodextrin (CD) moieties adds\nhydrophobic drug-complexing sites. Polyamidoamines (PAAs) are biocompatible and biodegradable\npolymers apt to create CD moieties in hydrogels. In this work, Ã?² or Ã?³-CD/PAA nanogels have been\ndeveloped. In vitro studies showed that a pretreatment for 24ââ?¬â??48 h with dexamethasone-loaded,\nÃ?²-CD/PAA nanogel (nanodexa) inhibits adhesion of Jurkat cells to human umbilical vein endothelial\ncells (HUVEC) in conditions mimicking inflammation. This inhibitory effect was faster and higher\nthan that displayed by free dexamethasone. Moreover, nanodexa inhibited COX-2 expression\ninduced by PMA+A23187 in Jurkat cells after 24ââ?¬â??48 h incubation in the 10âË?â??8ââ?¬â??10âË?â??5 M concentration\nrange, while dexamethasone was effective only at 10âË?â??5 M after 48 h treatment. Hence, the novel\nnanogel-dexamethasone formulation combines faster action with lower doses, suggesting the\npotential for being more manageable than the free drug, reducing its adverse side effects....
Mini-tablets are a great alternative for pellets and granules, because of their relative ease of manufacturing and dosage forms of equal dimensions, weight with smooth regular surface can be produced in a reproducible and continuous way. The main objective of the study was to develop and to evaluate encapsulated mini-tablets systems, in order to achieve desired target product profile for extended period of time. The drug-excipients compatibility study was carried out by FTIR and differential scanning colorimetry DSC. It was also observed that, all the parameters obtained were within specific limit of official compendia and hence complied with the standard. Depending on in-vitro disintegration time and % drug release up to 1 hr it was observed that formulation I3 containing 6% croscarmallose shown optimized result. The sustained release mini tablet into phosphate buffer pH 7.4 released 44.86% to 68.72% drug after 2 hr and the release rate was sustained upto 12th hr with slight variation in release rate. Maximum amount of drug was released by formulation S4 (99.08%). The study concluded that, mini-tablets is better alternative for the administration of different drug in different release pattern....
The aim of this study was to develop a novel folate receptor-targeted drug delivery\nsystem for retinoblastoma cells using a promising anticancer agent, curcumin-difluorinated (CDF),\nloaded in polymeric micelles. Folic acid was used as a targeting moiety to enhance the targeting and\nbioavailability of CDF. For this purpose, amphiphilic poly(styrene-co-maleic acid)-conjugated-folic\nacid (SMA-FA) was synthesized and utilized to improve the aqueous solubility of a highly\nhydrophobic, but very potent anticancer compound, CDF, and its targeted delivery to folate\noverexpressing cancers. The SMA-FA conjugate was first synthesized and characterized by 1H NMR,\nFTIR and DSC. Furthermore, the chromatographic condition (HPLC) for estimating CDF was\ndetermined and validated. The formulation was optimized to achieve maximum entrapment of CDF.\nThe particle size of the micelles was measured and confirmed by dynamic light scattering (DLS)\nand transmission electron microscopy (TEM). Cytotoxicity studies were conducted on (Y-79 and\nWERI-RB) retinoblastoma cells. Results showed that the solubility of CDF could be increased with the\nnewly-synthesized polymer, and the entrapment efficiency was >85%. The drug-loaded nanomicelles\nexhibited an appropriate size of <200 nm and a narrow size distribution. The formulation did not\nshow any adverse cytotoxicity on a human retinal pigment epithelial cell (ARPE-19), indicating its\nsafety. However, it showed significant cell killing activity in both Y-79 and WERI-RB retinoblastoma\ncell lines, indicating its potency in killing cancer cells. In conclusion, the folic acid-conjugated SMA\nloaded with CDF showed promising potential with high safety and pronounced anticancer activity\non the tested retinoblastoma cell lines. The newly-formulated targeted nanomicelles thus could be\na viable option as an alternative approach to current retinoblastoma therapies....
The objective of this research work was to formulate and evaluate of stomach specific chitosan based mucoadhesive microspheres of metoprolol tartrate by spray drying. The main drawback of metoprolol tartrate conventional dosage formulation are short biological half-life, its selective absorption form upper part of gastrointestinal tract, frequent administration and low oral bioavailability. By preparing chitosan based mucoadhesive microspheres of metoprolol tartrate, above drawbacks can be avoided. A 32 full factorial design was used for assessment of influence of two independent variable concentration of chitosan (X1) and polymer to drug ratio (X2) on the drug release at 6 hr (Y1) and 12 hr (Y2), % practical yield (Y3) and particle size (Y4). Mucoadhesive microspheres prepared by using spray drying because it gives better entrapment efficiency and small particle size with narrow particle size distribution. Microspheres was evaluated by various parameter with their results are entrapment efficiency (60.18-92.14%), mucoadhesion strength (68.8-83.9%), particle size (4.7-7.05 µm) and drug release at 12 hr (90.4-99.71%). Varying the concentration of chitosan and polymer to drug ratio have significant effect on response variables. Model validated by formulating the check point batch. No significant bias was found between predicted and observed value of check point batch. Short term stability study was carried out of optimized batch. The data of stability study revealed that the optimized formulation is stable. Hixon-Crowell model was fit to the drug release of optimized batch and its R2 value 0.9863....
Kafirin microparticles have potential as colon-targeted delivery systems because of their\nability to protect encapsulated material from digestive processes of the upper gastrointestinal tract\n(GIT). The aim was to optimize prednisolone loading into kafirin microparticles, and investigate\ntheir potential as an oral delivery system. Response surface methodology (RSM) was used to\npredict the optimal formulation of prednisolone loaded microparticles. Prednisolone release from the\nmicroparticles was measured in simulated conditions of the GIT. The RSM models were inadequate for\npredicting the relationship between starting quantities of kafirin and prednisolone, and prednisolone\nloading into microparticles. Compared to prednisolone released in the simulated gastric and small\nintestinal conditions, no additional drug release was observed in simulated colonic conditions.\nHence, more insight into factors affecting drug loading into kafirin microparticles is required to\nimprove the robustness of the RSM model. This present method of formulating prednisolone-loaded\nkafirin microparticles is unlikely to offer clinical benefits over commercially available dosage\nforms. Nevertheless, the overall amount of prednisolone released from the kafirin microparticles in\nconditions simulating the human GIT demonstrates their ability to prevent the release of entrapped\ncore material. Further work developing the formulation methods may result in a delivery system\nthat targets the lower GIT....
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