title: Pharmacokinetics and tissue distribution of spray-dried carboplatin microspheres: lung targeting via intravenous route.
abstract: For cancer therapy, microspheres can be used to increase effectiveness while decreasing side effects of treatments. We prepared gelatin microspheres containing carboplatin (GCPtM) for treating lung cancer. We prepared gelatin microspheres of carboplatin (GCPtM) for use in treating lung cancer. Microspheres were prepared using a Buchi B-90 nano spray-drier. Surface morphology was found to be shriveled to nearly spherical, with an average size of 14.7 μm. Drug loading and percentage yield were found to be 72 ± 0.4 and 88 ± 0.2 %, respectively. In vitro release studies indicated that diffusion followed the Peppas model, with 99.3 % of total carboplatin released from GCPtM after 12 h, while for the pure drug this value was 92.4 % in 0.5 h. Liquification was observed during stability studies at 37 °C with an relative humidity of 75 %. Plasma concentration profile was described using a two-compartment model after intravenous injection of GCPtM. Carboplatin containing microspheres distributed in the lung, spleen, liver, and blood were found to be primarily distributed in the lungs. We used a powder technology (spray-dryer) method in this study to significantly reduce the overall production time and desired particle size, without using organic solvents; additionally, this method is economically feasible. Thus, microsphere may be an effective method for successfully delivering carboplatin to the lungs.
authors.affiliation: Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi Arabia, sharsha@kfu.edu.sa.
authors.forename: Sree
authors.initials: S
authors.lastname: Harsha
authors.forename: Mohammed
authors.initials: M
authors.lastname: Al-Khars
authors.forename: Mohammed
authors.initials: M
authors.lastname: Al-Hassan
authors.forename: N Prem
authors.initials: NP
authors.lastname: Kumar
authors.forename: Anroop B
authors.initials: AB
authors.lastname: Nair
authors.forename: Mahesh
authors.initials: M
authors.lastname: Attimarad
authors.forename: Bandar E
authors.initials: BE
authors.lastname: Al-Dhubiab
mesh_terms: D000818:Animals; D016190:Carboplatin / Q000008:administration & dosage / Q000493:pharmacokinetics*; D016503:Drug Delivery Systems / Q000379:methods*; D005260:Female; D007262:Infusions, Intravenous; D008168:Lung / Q000187:drug effects* / Q000378:metabolism*; D008297:Male; D051379:Mice; D008863:Microspheres; D011897:Random Allocation; D014018:Tissue Distribution / Q000187:drug effects / Q000502:physiology
chemical_list: D016190:Carboplatin