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Colorectal cancer (CRC) is the third most common cancer leading to death worldwide following breast and lung cancer with the incidence rate of 10%. The treatment comprises surgery, radiation, and ablation therapy depending upon the stage of cancer.The review focuses on various drug delivery strategies explored to circumvent the major constraints associated with the conventional drug delivery systems-poor bioavailability, intra- and inter individual variability, exposure of normal cells to antineoplastic agents, and presence of efflux pump. All these attributes impact the effective delivery of chemotherapeutic agents at the tumor site. The various target specific drug delivery systems developed for colorectal cancer include pH-dependent, microbiologically triggered, time-dependent, magnetically driven, pressure-dependent, prodrug/polysaccharide-based, osmotic and ligand-mediated systems. This review enumerates novel target specific approaches developed and investigated for potential utility in CRC therapeutics.The limitations of conventional delivery systems can be overcome by the development of colon-specific targeted drug delivery systems that overcome the obstacles of nonspecific biodistribution, drug resistance, and unwanted adverse effects of conventional drug delivery systems. In addition, nanotechnology approaches help to increase drug solubility, bioavailability, reduce side effects, and provide superior drug response in CRC.

Heterocyclic compounds bearing the pyrimidine core are of tremendous interest as they constitute an important class of natural and synthetic compounds exhibiting diverse useful biological activities that hold attractive potential for clinical translation as therapeutic agents in alleviation of a myriad of diseases. Heterocycles possessing a pyrimidine scaffold have piqued tremendous interest of organic and medicinal chemists owing to their privileged bioactivities. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities. This heterocycle, being a significant endogenous component of the body, the pyrimidine derivatives can easily interact with enzymes, genetic materials, and bio components within the cell. The landscape of FDA approved drugs, presently marketed incorporating the pyrimidine scaffold continues to evolve in number and diversity. There is a tremendous surge in discovery of new targets across many diseases especially those involving emerging resistance to clinically used battery of drugs. Pyrimidine scaffolds will continue to be explored expanding their chemical space portfolio in an effort to find novel drugs impacting these targets. This review aims to provide an elaborate recapitulation of the recent trends adopted to synthesize propitious pyrimidine incorporated hits and also focuses on the clinical significance reported for functionalized pyrimidine analogues that would quintessentially aid medicinal chemists for new research explorations in this arena.

The present study reports the physicochemical, microbial and analytical (marker based) standardization of an Ayurvedic marketed formulation- Balaguloochyadi kashayam (Rajah Ayurveda). Physicochemical standardization was performed by determining organoleptic properties, pH, specific gravity and total solid content. Total bacterial count and total fungal count studies were performed for microbial standardization. Marker based standardization involved development and validation of a High Performance Thin Layer Chromatography (HPTLC) method for quantitative determination of a chemical marker viz. ephedrine present in Bala, major herb of Balaguloochyadi kashayam as per the standard protocols. The physicochemical and microbial tests were performed in triplicate and average results were calculated. A new, accurate, precise and robust HPTLC method for estimation of ephedrine in Balaguloochyadi kashayam was developed on Camag Linomat-5 using silica gel 60 GF254 as stationary phase and toluene: chloroform: n-propanol: ethanol: formic acid (6: 3: 1: 2: 1, v/v/v/v/v) as mobile phase. The validation studies were performed as per International Conference on Harmonization- Quality (ICH-Q2 (R1)) guidelines. The results of these experiments can be used by manufacturers as a reference for controlling the quality of Balaguloochyadi kashayam formulations prior to release for marketing.