The Journal of Pharmaceutics & Drug Delivery Research (JPDDR) promotes rigorous research that makes a significant contribution in advancing knowledge for Drug Delivery Research. The journal includes all major themes pertaining to Pharmaceutical Technology, Biopharmaceutics, Pharmacokinetics, and Molecular Drug Design.
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Preparation and Evaluation of Amino Acid Based Salt Forms of Model Zwitterionic Drug Ciprofloxacin
Ciprofloxacin (CIP) is a quinolone derivative which is widely used for the treatment of a number of urinary tract infections. It exhibits its antimicrobial activity by inhibiting bacterial DNA gyrase enzyme. BCS classification of CIP is challenging due to the absence of any linear dose proportionality of AUC in humans. Yet, most of the studies classify CIP as a BCS IV (low solubility & low permeability drug) candidate. This study aims at exploiting the zwitterionic nature of CIP and investigates the ability of acidic and basic amino acids to form new salts with the primary aim of improving its solubility. Two salts were prepared using L-glutamic acid and L-aspartic acid as counter ions which resulted in increasing CIP solubility by 2.9x103 and 2.5x103 folds respectively. On the other hand, cationic amino acids namely (L-arginine, L-lysine & L-histidine) failed to form any salts. To investigate the absence of salt formation with the cationic amino acids, the role of inter- and intra molecular interactions between CIP and amino acids on the salt formation was studied using molecular dynamic simulation. Both the experimental and theoretical results revealed that ionic and hydrophobic interactions are essential for salt formation and that the ionic interaction and/or hydrophilic interactions between CIP and amino acids molecules should be greater than hydrophobic interactions between CIP molecules. Future work will study the effect of the salts on the permeability behaviour of CIP across Caco-2 monolayers.
Population Pharmacokinetics of Lixisenatide, a Once- Daily Human Glucagon-Like Peptide-1 Receptor Agonist, in Healthy Subjects and in Patients with Type 2 Diabetes
Lixisenatide is a potent and selective glucagon-like peptide-1(GLP-1) receptor agonist developed for the treatment of type 2 diabetes (T2DM) with a subcutaneous once-daily regimen. The substance is currently under review for marketing authorization for the management of T2DM. In this study, the population pharmacokinetics in healthy volunteers and in adult T2DM patients was investigated.
Characterization of Ethylcellulose and Hydroxypropyl Methylcellulose Microspheres for Controlled Release of Flurbiprofen
The objective of this study was to design and optimize polymeric microspheres of flurbiprofen (FLB) with ethylcellulose (EC) and hydroxypropyl methylcellulose (HPMC) using response surface methodology. EC and HPMC were taken as independent variables whereas; the dependent variables were % drug release at pH 1.2, 4.5 and 7.4. FTIR spectra and TGA showed no significant difference between drug and polymers. DSC and XRD studies exhibited molecular dispersion of FLB within microspheres. Contour plots were drawn to predict the relationship between dependent and independent variables. Both polymers revealed their significant effects on drug release that followed the zero order which was further verified by the lowest values of Akaike information criterion. The mechanism of drug release followed super case II type of drug release. This study helped unraveling the influence of two factors on in-vitro drug release and thereby, proposed an appropriate sustained drug release formulation.