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Preparation, Optimization, and In Vivo Evaluation of Nanoparticle-Based Formulation for Pulmonary Delivery of Anticancer Drug

Wockhardt Research Centre, D-4, M.I.D.C., Chikalthana, Aurangabad (M.S) 431006, India
Dr. Prabhakar Kore Basic Science Research Centre, KLE Academy of Higher Education and Research, Belagavi 590010, Karnataka, India
KLE University’s College of Pharmacy, KLE Academy of Higher Education and Research, Nehru Nagar, Belagavi 590010, Karnataka, India
Department of Pharmaceutics, Y.B. Chavan College of Pharmacy, Zakaria Campus, Aurangabad (M.S) 431001, India
Author to whom correspondence should be addressed.
Medicina 2019, 55(6), 294;
Received: 5 May 2019 / Revised: 11 June 2019 / Accepted: 18 June 2019 / Published: 20 June 2019
(This article belongs to the Special Issue Nano-Biosciences in the Field of Health-Care)
PDF [10654 KB, uploaded 26 June 2019]


Background and Oobjectives: Lung cancer, a pressing issue in present-day society due to its high prevalence and mortality rate, can be managed effectively by long-term delivery of anticancer agents encapsulated in nanoparticles in the form of inhalable dry powder. This approach is expected to be of strategic importance in the management of lung cancer and is a developing area in current research. In the present investigation, we report on the formulation and characterization of docetaxel inhalable nanoparticles as a viable alternative for effective treatment of non-small cell lung cancer as a long-term delivery choice. Materials and Methods: Poloxamer (PLX-188) coated poly(lactic-co-glycolic acid) (PLGA) nanoparticles containing docetaxel (DTX-NPs) were prepared by simple oil in water (o/w) single emulsification-solvent evaporation process. The nanoparticles were collected as pellet by centrifugation, dispersed in mannitol solution, and lyophilized to get dry powder. Results: Optimized DTX-NPs were smooth and spherical in morphology, had particle size around 200 nm, zeta potential around −36 mV, and entrapment efficiency of around 60%. The in vitro anticancer assay was assessed and it was observed that nanoparticle-based formulation exhibited enhanced cytotoxicity when compared to the free form of the drug post 48 h. On examining for in vitro drug release, slow but continuous release was seen until 96 h following Higuchi release kinetics. DTX-NPs were able to maintain their desired characteristics when studied at accelerated conditions of stability. Conclusions: In-vivo study indicated that the optimized nanoparticles were well retained in lungs and that the drug level could be maintained for a longer duration if given in the form of DTX-NPs by the pulmonary route. Thus, the non-invasive nature and target specificity of DTX-NPs paves the way for its future use as a pulmonary delivery for treating non-small cell lung cancer (NSCLC). View Full-Text
Keywords: PLGA nanoparticles; Lyophilization; non-small cell lung cancer; pulmonary PLGA nanoparticles; Lyophilization; non-small cell lung cancer; pulmonary

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Chishti, N.; Jagwani, S.; Dhamecha, D.; Jalalpure, S.; Dehghan, M.H. Preparation, Optimization, and In Vivo Evaluation of Nanoparticle-Based Formulation for Pulmonary Delivery of Anticancer Drug. Medicina 2019, 55, 294.

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