Preparation and evaluation of inhaled dry powders based on folic acid-conjugated Docetaxel nanoparticles

Abstract

Abstract:

AIM: To prepare docetaxel-loaded folic acid-conjugated nanoparticles (NPs-DTX-FA) for the treatment of lung cancer. METHODS: The NPs-DTX-FA were prepared by the solvent evaporation method and the nanoparticles (NPs) were then co-spray dried with excipients to obtain inhaled dry powders. The physiochemical properties of NPs and inhaled dry powders were evaluated. MTT assay was employed to study the cytotoxicity and tumor-targeting property of the NPs. RESULTS:The diameter of LPs-DTX-FA was （100.1±1.0） nm, the IC50for NPs-DTX and NPs-DTX-FA were （2.09±0.82） μmol/L and （0.80±0.32） μmol/L, respectively. The fine particle fraction (FPF) and angle of repose (θ) of the inhaled dry powders were （21.10±0.18）% and （36.75±0.52）°, respectively. CONCLUSION: The preparation of NPs-DTX-FA based inhaled dry powders was successful and this formulation represented a possibility of clinical application by achieving higher anti-cancer activity in tumor site and lower damage to healthy organs.

Key words: docetaxel, nanoparticle, dry powder inhalation

CLC Number:

R965.2

ZHU Xiaojie, KONG Ying, LIU Qi, LU Yang, ZHAO Di, LI Ning, CHEN Xijing . Preparation and evaluation of inhaled dry powders based on folic acid-conjugated Docetaxel nanoparticles[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2017, 22(5): 495-500.

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