title: Venlafaxine loaded chitosan NPs for brain targeting: pharmacokinetic and pharmacodynamic evaluation.
abstract: The purpose of the present investigation was to prepare venlafaxine (VLF) loaded chitosan nanoparticles (NPs) to enhance the uptake of VLF to brain via intranasal (i.n.) delivery. VLF loaded chitosan NPs were prepared and characterized for particle size, size distribution, zeta potential, encapsulation efficiency and in vitro drug release. In order to investigate the localization of chitosan NPs in brain and other organs qualitatively confocal laser scanning microscopy technique was carried out using rhodamine-123 (ROD-123) as marker. The levels of VLF in plasma and brain tissues were also determined, the brain/blood ratios of VLF for VLF (i.v.), VLF (i.n.), VLF chitosan NPs (i.n.) were 0.0293, 0.0700 and 0.1612, respectively, at 0.5h, indicative of better brain uptake of VLF chitosan NPs. The higher drug transport efficiency (508.59) and direct transport percentage (80.34) of VLF chitosan NPs as compared to other formulations suggest its better efficacy in treatment of depression.
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, Hamdard Nagar, New Delhi 110 062, India; Ranbaxy Research Laboratories, Gurgaon, India.
authors.forename: Shadabul
authors.initials: S
authors.lastname: Haque
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, Hamdard Nagar, New Delhi 110 062, India.
authors.forename: Shadab
authors.initials: S
authors.lastname: Md
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, Hamdard Nagar, New Delhi 110 062, India.
authors.forename: Mohammad
authors.initials: M
authors.lastname: Fazil
authors.affiliation: Advanced Instrumentation Research Facility, Jawaharlal Nehru University, New Delhi, India.
authors.forename: Manish
authors.initials: M
authors.lastname: Kumar
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, Hamdard Nagar, New Delhi 110 062, India.
authors.forename: Jasjeet Kaur
authors.initials: JK
authors.lastname: Sahni
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, Hamdard Nagar, New Delhi 110 062, India.
authors.forename: Javed
authors.initials: J
authors.lastname: Ali
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, Hamdard Nagar, New Delhi 110 062, India.
authors.forename: Sanjula
authors.initials: S
authors.lastname: Baboota
mesh_terms: D000281:Administration, Intranasal; D000818:Animals; D018687:Antidepressive Agents, Second-Generation / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D001522:Behavior, Animal / Q000187:drug effects; D001921:Brain / Q000378:metabolism*; D048271:Chitosan / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D003511:Cyclohexanols / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D004339:Drug Compounding; D005260:Female; D066298:In Vitro Techniques; D008297:Male; D009043:Motor Activity / Q000187:drug effects; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry; D009297:Nasal Mucosa / Q000378:metabolism; D017208:Rats, Wistar; D000069470:Venlafaxine Hydrochloride
chemical_list: D018687:Antidepressive Agents, Second-Generation; D003511:Cyclohexanols; D000069470:Venlafaxine Hydrochloride; D048271:Chitosan