Priyanka Verma

Dipeptidyl peptidase IV is a key regulator of insulin- stimulating hormones, glucagon-like peptide and glucose dependent insulinotrophic polypeptide. Thus it is a promising target for treatment of type 2 Diabetes mellitus. Inhibition of plasma Dipeptidyl peptidase IV enzyme lead to enhanced endogenous glucagon like peptide-1, GIP activity which ultimately results in the potentiating of insulin secretion by pancreatic cell and subsequent lowering blood glucose level, HbA [1c], glucose secretion, liver glucose production. One of the principal goals of diabetes management is to attain haemoglobin HbA [1c] treatment goals and prevent the onset or decrease the rate of occurrence of Microvascular conditions.2, 6 numerous treatment options are available for management of Type 2 Diabetes mellitus, various class of DPP IV inhibitor being explored such as Sitagliptin and Vildagliptin successfully launched. Several other novel DPP IV inhibitors are in pipeline, Unless there are clear contraindications, metformin monotherapy is prescribed, and if HbA [1c] targets are not attained after 3 months, 1 of several classes of agents could be added, such as sulfonylurea’s, Thiazolidinediones, dipeptidyl peptidase-4 inhibitors, - glucagon like peptide-1 receptor agonists, or basal insulin.2,6 Despite the broad range of therapeutic options, the attainment of HbA [1c] goals among patients with diabetes remains challenging, with just slightly more than half (52%) of diabetes patients attaining the common HbA [1c] goal of < 7.0%. The present review summarizes latest preclinical and clinical trial data of different DPP IV inhibitors with a special emphasis on their DPP8/9 fold selectivity and therapeutic advantages over GLP-1 based approach. Keywords: Diabetes 2, Dipeptidyl Peptidase-4, glucose-dependent insulinotrophic polypeptide, glucagon-like peptide-1.

Liquisoild technique is a novel concept for delivery of drugs through oral route. This approach of delivering drugs is suitable mostly for lipophilic drugs and poorly or water insoluble drugs. With this approach sustained release formulation of hydrophilic drugs or freely water soluble drug can also be prepare. Release enhancement of poorly soluble drugs is achieved by choosing nonvolatile solvent with maximum drug solubility, Unlike this, in retardation of drug release nonvolatile solvent with lowest drug solubility is choosen. It was found from the study that if nonvolatile solvent alone is not sufficient for prolonging the drug release then various release retarding agent is used. The release retarding or sustained release agent used, may be of natural or synthetic origin.

Clotrimazole (CLTZ) is a local imidazolic antifungal agent. A major problem associated with the successful formulation of effective dosage forms containing CLTZ is its poor aqueous solubility, which presents a hindrance for the local availability of CLTZ and limits the effective antifungal therapy. In the present study, the effects of various concentrations of poly(amidoamine) (PAMAM) dendrimers generation 3.5 (G3.5) and generation 4 (G4) with carboxylate (DCC), amine (DCN) and hydroxyl surface groups (DCO) on aqueous solubility, in vitro drug release studies, and for stability studies of CLTZ drug. The obtained results showed that all tested PAMAM dendrimers improved the solubility of CLTZ and the more potent were (DCC) dendrimers. The increase in solubility of CLTZ was highest at dendrimer concentration of 10 mg/ml. These observations indicate that PAMAM dendrimers enhance the solubility of CLTZ, The drug dendrimers complexes displayed the controlled release action during in vitro release studies. Formulation with amine and carboxylate were subjected to accelerated stability studies. Key words: poly(amidoamine) dendrimers; clotrimazole; aqueous solubility; surface groups