Nanocrystals: A Deep Insight into Formulation Aspects, Stabilization Strategies, and Biomedical Applications.

BACKGROUND: Drugs with poor solubility exhibit hurdles in their formulation due to poor dissolution and low bioavailability. Nanocrystallization is a great technique for incorporating poorly soluble drugs and is associated with many benefits. OBJECTIVE: The objective of the present review is to discuss formulation techniques for the generation of Nanocrystals (NCs) and illustrate the various advantages of NCs. It also explains commonly used stabilizers and guidelines for their safe use for enhancing NCs and provides a deep insight into various biomedical applications of NCs. METHODS: The review was extracted from the study carried out in the general literature to emphasize the importance of NCs in various formulations. RESULTS: NCs are a widely accepted approach to enhancing drug solubility. There are so many marketed products of nanocrystal drug formulations that are being used to treat life-threatening disorders. Two techniques can be used to formulate NCs, i.e., the bottom-up method and the top-down method. Their main biomedical applications are found in oral, parenteral, pulmonary, ocular, dermal, and mucosal formulations. CONCLUSION: In the present review, different formulation methods of NCs have been discussed in detail, followed by explaining the advantages and various targeted drug delivery systems covered by NCs formulations. The development of NCs-based formulation avoids the limitations of other systems used for targeted drug delivery.

Synthesis and biological profile of substituted benzimidazoles.

BACKGROUND: A series of benzimidazole derivatives was developed and its chemical scaffolds were authenticated by NMR, IR, elemental analyses and physicochemical properties. The synthesized compounds were screened for their antimicrobial and antiproliferative activities. RESULTS AND DISCUSSION: The synthesized benzimidazole compounds were evaluated for their antimicrobial activity using the tube dilution method and were found to exhibit good antimicrobial potential against selected Gram negative and positive bacterial and fungal species. The compounds were also assessed for their anticancer activity exhibited using the SRB assay and were found to elicit antiproliferative activity against MCF7 breast cancer cell line, which was comparable to the standard drug. CONCLUSION: Antimicrobial screening results indicated that compounds 1, 2 and 19 to be promising antimicrobial agents against selected microbial species and comparable to standard drugs which included norfloxacin and fluconazole. The anticancer screening results revealed that compounds, 12, 21, 22 and 29 to show the highest activity against MCF7 and their IC50 values were more potent than 5-fluorouracil.

Analgesic, anti-inflammatory and antiulcer activity of nitric oxide releasing ester derivatives of indomethacin.

Analgesic, antiinflammatory and antiulcer activity of newly synthesized nitric oxide (NO) releasing ester derivatives of indomethacin were evaluated in rats. Synthetic compounds (NB-02, NP-02 and NE-02) 6 mg/kg, po each significantly (P < 0.01) increased the tail flick reaction time in rats. Antinociceptive effects of two derivatives (NB-02 and NE-02) were compared to that of the parent compound. Indomethacin derivatives (NB-02, NP-02 and NE-02) exhibited significant (P < 0.01) anti-inflammatory activity as observed in carrageenan induced rat paw inflammatory model. The severity of gastric lesion were also significantly (P < 0.01) less in animals treated with ester derivatives of indomethacin (NB-02, NP-02 and NE-02) as compared to mo-control.