title: Controlled release studies of antimalarial 1, 3, 5-trisubstituted-2-pyrazolines from biocompatible chitosan-heparin Layer-by-Layer (LbL) self assembled thin films.
abstract: Herein we report the in-vitro controlled release properties of 1, 3, 5-trisubstituted-2-pyrazolines through Layer-by-Layer (LbL) self assembled thin films fabricated from chitosan and heparin sodium salt as biocompatible polyelectrolytes. This study was carried out as a preliminary step towards the applicability of LbL technique in prophylactic drug delivery of antimalarial drugs. The growth of LbL self assembly was monitored by UV-Visible spectrophotometry and Quartz Crystal Microbalance (QCM). The loading as well as in-vitro release studies (in phosphate buffer saline at pH 7.4) were carried out using UV-Visible spectroscopy. Three compounds having good antimalarial activity were tested and the release rate was found inversely proportional to the hydrophobicity of the drug. Pzln-4 has shown best release among all the three compounds (up to 780 min) followed by Pzln-5 and Pzln-8. The release trend was that of a fast release up to first 2 h followed by a steady release. Kinetic fitting of the data confirmed the process of drug release followed a pseudo second order kinetics (R(2)≥0.99). A large value of rate constant (k) revealed a faster release. Pzln-4 has shown smallest value of k corresponding to slowest release among all the three compounds.
authors.affiliation: Process Technology Development Division, Defence R & D Establishment, Jhansi Road, Gwalior, Madhya Pradesh, 474002, India.
authors.forename: Uma M
authors.initials: UM
authors.lastname: Bhalerao
authors.affiliation: Process Technology Development Division, Defence R & D Establishment, Jhansi Road, Gwalior, Madhya Pradesh, 474002, India.
authors.forename: Aditya Kapil
authors.initials: AK
authors.lastname: Valiveti
authors.affiliation: Process Technology Development Division, Defence R & D Establishment, Jhansi Road, Gwalior, Madhya Pradesh, 474002, India. Electronic address: jracharya01@gmail.com.
authors.forename: Jyotiranjan
authors.initials: J
authors.lastname: Acharya
authors.affiliation: School of Studies in Chemistry, Jiwaji University, Gwalior, Madhya Pradesh, 474011, India.
authors.forename: Anand K
authors.initials: AK
authors.lastname: Halve
authors.affiliation: Process Technology Development Division, Defence R & D Establishment, Jhansi Road, Gwalior, Madhya Pradesh, 474002, India.
authors.forename: Mahabir Parshad
authors.initials: MP
authors.lastname: Kaushik
mesh_terms: D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry*; D001672:Biocompatible Materials; D002021:Buffers; D048271:Chitosan / Q000737:chemistry*; D003692:Delayed-Action Preparations / Q000737:chemistry*; D065546:Drug Liberation; D006493:Heparin / Q000737:chemistry*; D057927:Hydrophobic and Hydrophilic Interactions; D007700:Kinetics; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry*; D058525:Quartz Crystal Microbalance Techniques; D012996:Solutions
chemical_list: D000962:Antimalarials; D001672:Biocompatible Materials; D002021:Buffers; D003692:Delayed-Action Preparations; D011720:Pyrazoles; D012996:Solutions; D006493:Heparin; D048271:Chitosan
keywords: Antimalarials; Biocompatible; Controlled release; Polyelectrolytes; Quartz crystal microbalance