In the present study, the main problem of cancer chemotherapy is the severe toxic side effects of anticancer drugs on healthy tissues that impose dose reduction, treatment delay along with health risks like hair loss, nausea and a major damage to the patient‘s immune system. The cancer drugs that are recommended in the second-line cancer chemotherapy, methotrexate (MTX) is considered as one of the most versatile drugs used in several types of cancer e.g. breast, head and neck and osteosarcoma along with rheumatoid arthritis, for delivery of MTX by parenteral or oral route is the poor bioavailability due to the limited absorption of the drug. In the current study ceramic-based nanoparticles layered double hydroxides (LDH) was synthesized by simple laboratory based wet chemical method (coprecipitation) and a well-known anticancer agent methotrexate (MTX) was intercalated by ex-situation exchange techniques to develop drug intercalated ceramic nanohybrid, abbreviated as LDH-MTX. The LDH-MTX nanohybrid was encapsulated with an approved biodegradable and biocompatible polymer poly (lactic-coglycolic acid) (PLGA) by double emulsion-solvent evaporation(W1/O/W2) techniques as well and was optimized by keeping some of the process parameters constant, while other process and formulation parameters e.g. the homogenization speed, concentration of polymer (PLGA), LDH-MTX and surfactants, aqueous and organic phase volume involved in the synthesis of the PLGA-LDH-MTX nanohybrids, were varied and evaluated to obtain the desired particle size range ~200nm and drug entrapment efficiency for specific use, this could be beneficial to realize the passive tumor-targeted drug delivery through enhanced permeability and retention (EPR) effects. The optimized drug-containing nanohybrids xxiv (PLGA-LDH-MTX) showed a sustained release profile till 240h (10days).
Dexamethasone is a glucocorticoid medication. This study was to develop guar gum-basedcolon targeted tablets of dexamethasone in the prevention of inflammatory bowel disease (IBD). The powder mix was subjected to micrometric evaluation (like bulk density and Carr's index) and drug content uniformity. Powder mix showed high values of Carr's index indicating low compressibility and drug content uniformity tests how uniformity of drug content that proved mixing uniformity. Matrix tablets containing 40% (DX-40), 50% (DX-50), 60% (DX-60), 70% (DX-70) and 80% (DX-80) of guargum were prepared by directcompression technique. Dexamethasone matrix tablets containing various proportions of guargum ranging from 40 to 80% of guar gum were subjected to measurement of mass degree ofswelling and gel strength. This indicates that swelling of the guargum-based formulations isincreasing as percentage of guargum is increasing. When subjected to post compression evaluation like hardness and friability formulations DX-70 and DX-80 containing 70% and 80% of guargum respectively showed very low hardness and friability 1.67 and 0.43kg/cm2respectively. Hence, further studies like in-vitro release studies, scanning electron microscopy (SEM) and short-term stability study were not conducted on these formulations. Formulation DX-40 containing 40% of guargum released about 87% of its drug content within 18 h in the physiological environment ofcolon. This may result in the release of drug in the last part of the small intestine itself. The tablet formulation DX-50 containing 50% of guargum also release about 88% of drug contentin the physiological environment of colon at the end of 24hrs of the study. However, at theend of 24 hour dissolution study, the matrix tablets of dexamethasone DX-60 containing 60% of guar gum released about 58% of the drug in the physiological environment of colon.
S. Kannan, S. Pratheepa*, P. Perumal, S. Selvaraj.