Objective: Gefitinib, Epidermal Growth Factor-Tyrosine Kinase Inhibitor (EGFR-TKI); has promisingly shown activity against Non-Small-Scale Lung Cancer. Currently, the formulations of this drug available are in Tablets, Capsules and liposomal suspensions taken by the oral route. These have certain disadvantages in gastrointestinal disorders like irritation of GI mucosal layer, bleeding, non-patient compliance and low bioavailability due to low aqueous solubility and thus low bioavailability. The purpose of this study was to formulate and evaluate Chitosan-based Microparticles of Gefitinib for maintaining the therapeutic index and limits its side effects.Methods: Chitosan microspheres cross-linked with glutaraldehyde were prepared by solvent evaporation technique which is then analyzed for its particle size, encapsulation efficiency, swelling index.Results: The release rate of the drug can be increased by using chitosan-based carrier system which will enhance its bioavailability. By this work, the anticancer activity of Gefitinib in non-small-scale lung cancer will be successfully determined.Conclusion: It has been concluded that microspheres can be prepared by solvent evaporation technique by varying the concentration of chitosan and tween-20. Chitosan used in this work is of 85 % degree of deacetylation, 25 % solution of Gluteraldehyde suitable for the formulation of these microspheres. Optimized temperature was selected as 65 °C, and the rotation speed was taken as 1200 rpm. Finally, the objectives planned for this research work was performed and evaluated and shown promising results as the dosing frequency is reduced and maximize for 3 d rather than once in a day as per the current formulation available in the market now with a low dosage regimen of 100 mg of dosage strength, administer by pulmonary route. Microparticulate drug delivery system from microspheres is able to deliver the drug in a sustained release manner for the long period of time successfully.
Objective: The aim of the present study is to develop docetaxel-loaded nano liquid crystals (NLCs) to enhanced and effective delivery of the drug to the skin cancer. Methods: NLCs bearing docetaxel were prepared by an emulsification solvent diffusion method. The formulated NLCs were characterized for average particle size, polydispersity index (PDI) Zeta potential, entrapment efficiency and in vitro drug release study. The prepared formulations were studied for it's in vitro cell line and cell uptake study. Results: It was revealed that the average size of NLCs was found 178.3±5.07, PDI was 0.189, percent entrapment efficiency was found 71.3±2.49 and Zeta potential was found-17.3±2.4. In vitro release determined by Franz diffusion cell was found 61.6±3.2% after 72 hr. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay shows that Docetaxel loaded NLCs were giving more cytotoxicity as compared to the plain drug. The cell uptake study was found enhanced uptake of fluorescein isothiocyanate (FITC) loaded NLCs in comparison to plain FITC. Docetaxel and docetaxel-loaded NLCs showed 28.3±0.3 and 39.3±1.3 growth inhibition respectively after 48h upon incubation at 0.5 µg/ml concentration (p<0.05). Conclusion: The result of the studies was concluded that NLCs can be used as impending drug delivery system which may enhance the drug uptake and maintain the drug level for longer period of time and it is potential carrier system which can be used for the treatment of skin diseases like cancer.
Herpes Simplex Keratitis (HSK), which is a major reason of corneal infection. The virus (Herpes simplex virus) enters into a latent phase. It presents primary infection as conjunctiva and eyelids swelling and mild inflammation. According to global research of disease, it is around 1.4 million, including 38,000 new cases of visual impairment or blindness every year. Several oral and topical antiviral drugs for HSK are out there commercially. However, toxicity and low patient compliance hamper use in HSK. Thus, an effective and safe delivery for HSK is required. The conventional ocular delivery systems such as suspension, solutions and ointments show drawbacks like increased low efficiency, pre-corneal elimination and blurred vision respectively, resulting to poor bioavailability. Ophthalmic In-situ gels, which are viscous polymer-based liquids are instilled in eyes as drops that undergoes sol-to-gel transition that improve duration of corneal contact and ocular bioavailability and thereby reducing frequency of administration. Merits of Ophthalmic in-situ gels over conventional dosage forms are possibility of releasing drugs at constant and slow rate with increased ocular residence time, increased shelf life and accurate dosing. This research includes ion induced in-situ-forming polymeric systems using combination of gelling agents to prolong corneal contact time, eradicate drug elimination and increase the bioavailability.
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