Docetaxel-Loaded Chitosan Microspheres as a Lung Targeted Drug Delivery System: In Vitro and in Vivo Evaluation

Abstract

The aim of this study was to prepare docetaxel-loaded chitosan microspheres and to evaluate their in vitro and in vivo characteristics. Glutaraldehyde crosslinked microspheres were prepared using a water-in-oil emulsification method, and characterized in terms of the morphological examination, particle size distribution, encapsulation ratio, drug-loading coefficient and in vitro release. Pharmacokinetics and biodistribution studies were used to evaluate that microspheres have more advantage than the conventional formulations. The emulsion crosslinking method was simple to prepare microspheres and easy to scale up. The formed microspheres were spherical in shape, with a smooth surface and the size was uniform (9.6 ± 0.8 μm); the encapsulation efficiency and drug loading of prepared microspheres were 88.1% ± 3.5% and 18.7% ± 1.2%, respectively. In vitro release indicated that the DTX microspheres had a well-sustained release efficacy and in vivo studies showed that the microspheres were found to release the drug to a maximum extent in the target tissue (lung). The prepared microspheres were found to possess suitable physico-chemical properties and the particle size range. The sustained release of DTX from microspheres revealed its applicability as drug delivery system to minimize the exposure of healthy tissues while increasing the accumulation of therapeutic drug in target sites.

<p>An Efficient, Lung-Targeted, Drug-Delivery System To Treat Asthma Via Microparticles</p>

“…These microspheres are obtained from spray-drying techniques, and the results of this study are also supported by other researchers. 61,62 Both drug-distribution schemes (ie, with SPP and conventional approaches) indicate that the organ/tissue is exposed to the drug to a greater extent if the Re (drug exposure) value is >1. The lungtargeting efficacy (Te) of the SPP formulation and the conventional formulation are shown in Table 4.…”

Tackling the Problem of Tuberculosis by Nanotechnology

“…Nanospheric particles as drug delivery systems are gaining increasing interest in the biomedical field. Nanospheres and microspheres are also found to be efficient drug delivery systems for intravenous administration because of their comparatively long bloodstream circulation (Hire and Derle, 2014;Wang et al, 2014). It was expected that when the drugs are released after internalization of micelle, by cleavage, they act as pro-drugs and enhance solubility of hydrophobic drugs, reduce drug toxicity, increase bioavailability, specificity, and systematic release of drugs, and prolong the drug action (Moghimi et al, 1993;Croy and Kwon, 2006;Dadwal, 2014).…”

Sophoridine-loaded PLGA microspheres for lung targeting: preparation, in vitro, and in vivo evaluation

“…These results indicated that the microspheres could deliver SRI predominantly to lung tissue after i.v. administration, which is preferable for the treatment of lung cancer, and the reduction of side effects as well (Madan et al, 2013;Wang et al, 2014).…”