Objective: DPP-4 (Dipeptidyl peptidase-4) inhibitors are the oral antidiabetics that inhibits the enzyme DPP-4. The main aim of study was to formulate, statistically optimize and characterize the polymeric nanomicellar (PNM) formulation of DPP-4 inhibitor (sitagliptin) using natural polymer and a non-ionic surfactant. Method: Response surface methodology (RSM) an experimental design was applied for optimization of nanomicelles using full central composite design. Drug and polymer concentration are independent variables (each at two factor three level) whereas drug loading (% DL) (R1), entrapment efficiency (% EE) (R2) and % drug release (R3) were identified as dependent variables. The polymeric nanomicelles were prepared by direct dissolution method and characterized for surface morphology, particle size, polydispersity index, zeta potential, entrapment efficiency, drug loading and % drug release. Results: The optimized formulation of sitagliptin loaded polymeric nanomicelles (PNM 10) was found to be clear, homogenous nanomiceller solution with round spherical structures with a low poly dispersity index of 0.564. PNM 10 has particle size of 368.2 nm. PNM 10 showed drug loading of 38.67 ± 0.23%, entrapment efficiency of 79.67 ± 0.54% and % drug release (R3) of 82.34 ± 0.78%. Conclusion: Design- Expert (DOE) version 11.0.5.0 software (Stat-Ease Inc, USA) was used for statistically optimization of formulations. PNM 10 was considered best optimized formulation and highly stable for prolonged use and found to be safe for application. Thus this can be a futuristic approach for developing nanomicelles, which can minimize the possible side effects of drug.
10 April 2020 in Mini-Reviews in Medicinal Chemistry
The current trend of increment in the frequency of antifungal resistance has brought research into an era where new antifungal compounds with novel mechanisms of action are required. Natural antimicrobial peptides, which are ubiquitous components of innate immunity, represent their candidature for novel antifungal peptides. Various antifungal peptides have been isolated from different species ranging from small marine organisms to insects and from various other living species. Based on these peptides, various mimetics of antifungal peptides have also been synthesized using non-natural amino acids. Utilization of these antifungal peptides is somehow limited due to their toxic and unstable nature. This review discusses recent updates and future directions of antifungal peptides, for taking them to the shelf from the bench.
10 April 2018 in Recent Advances in Drug Delivery and Formulation
Background: Neurodegenerative disorders are one of the common diseases that affect our society with tremendous medical and financial burdens. As a whole, neurodegeneration affects individuals of all ages, but becomes increasingly frequent with age, coming to affect a very large share of our elderly population which is severely affecting the patient, caregivers, and enormously increasing the financial burden of the nation. These diseases share a very complex nature, which often result from combined genetic, environment and pathogenic factors. Various challenges are faced by the scientific community that researches on the pathogenesis and the therapy of neurodegenerative disorder. Objective: The review has been analysed for recent patent documents and treatment approaches for neurodegenerative disorders. Method: The study design is based on updating the international and national literatures and an exhaustive patent search and compiling of various patented documents for the treatment of neurodegenerative disorders (EP2282779 A1, US20110229555 A1) to provide information in the state of technological innovation in terms of research and development. Results: In the present review, the authors described various neurodegenerative diseases, there treatment strategies and emphasized on various patented approaches for age-related neurodegenerative disorders such as New therapeutic approaches for treating Alzheimer disease and related disorders through a modulation of cell stress response EP2282779 A1, through combined therapies that modulate angiogenesis US20120058992 A1. Conclusion: The review will attract the interest of academics, researchers, students and pharmaceutical companies in the recent on-going activities in neurodegenerative disorders.
Objective: The main objective of the study was to develop gliptin loaded polymeric nanomicelles by direct dissolution method. The comparative evaluation studies were performed to study the effect of polymer concentration on particle size, entrapment efficiency, loading capacity and drug release of the formulation. Methods: Gliptin loaded polymeric nanomicelles were prepared by the direct dissolution method. The formulations were prepared by varying the concentration of polymer and drug concentration was kept constant in all the formulations. The concentration of polymer (pullulan) was maintained 0.1%, 0.5% 1% in formulation F-1, F-2 and F-3, respectively. The effect of polymer concentration on mean particle size, zeta potential, % entrapment efficiency, % loading capacity and in vitro drug release was studied. Results: The optimized nanoformulation was obtained with pullulan 0.1% concentration with a mean particle diameter of 368.2nm and zeta potential value (-7.96mV) indicating greater stability. Conclusion: Hence F-1 was considered to be the best formulation for the preparation of gliptin loaded polymeric nanomicelles. Hence, it can be concluded that polymeric nanomicellar approach can be beneficial to improve the bioavailability and poor permeability of class III drugs like gliptins and thus can be a better approach for controlled drug delivery.
Targeted drug delivery systems that selectively deliver anticancer drugs to tumour cells have always been a field of interest to reduce side effects associated with chemotherapy in cancer patients. Cancer cells require nutrients for their multiplication; folic acid is one such nutrient. Expression of folate receptors is negligible in normal cells, whereas they are overexpressed in a variety of cancer cells. A number of studies have shown that selective targeting of folate receptors in cancer is a beneficial approach, as folate targeted anticancer conjugates are selective towards cancer cells, thereby sparing non-cancerous cells. In this review, we have discussed folate receptor, folic acid as a cancer targeting moiety, different folate targeted anticancer drug conjugates, and different folate conjugated nanodelivery systems. This summarized information may turn out to be valuable for researchers to design novel folate targeted anticancer drug delivery systems having the potential to reduce the drawbacks associated with conventional cancer therapeutics.