Preparation and Characterization of Spray-Dried Inhalable Powders Containing Polymeric Micelles for Pulmonary Delivery of Paclitaxel in Lung Cancer

Authors

  • Mahboubeh Rezazadeh Department of Pharmaceutics and Novel Drug Delivery System Research Center , School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences , Isfahan.
  • Zahra Davatsaz Department of Pharmaceutics , School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences , Isfahan.
  • Jaber Emami Department of Pharmaceutics , School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences , Isfahan.
  • Farshid Hasanzadeh Department of Pharmaceutics , School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences , Isfahan.
  • Ali Jahanian-Najafabadi Department of Pharmaceutical Biotechnology , School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences , Isfahan.

DOI:

https://doi.org/10.18433/jpps30048

Abstract

Purpose: Local delivery of chemotherapeutic drugs to the lungs offers many advantages for lung cancer treatment compared to conventional systemic chemotherapy. In the present study, novel mixed polymeric micelles based on tocopheryl succinate-polyethylene glycol 1000 and 5000 Da (TPGS1K and TPGS5K) were synthesized and loaded with paclitaxel (PTX). Then, the optimized micelles were incorporated as colloidal drug delivery system into lactose carrier particles using a spray drying technique. Methods: The mixed micelles of TPGS5K and TPGS1K in different molar ratios (10:0, 7:3, 5:5, 3:7, 0:10) were prepared and physicochemical properties including: particle size, zeta potential, critical micelle concentration (CMC), drug loading, drug release rate, and in vitro cytotoxicitywere investigated in details. The optimized nanoparticles were co-spray dried with lactose carriers to produce the spherical particle morphology of the inhalable particles. Results: Particle sizes and zeta potentials of the different formulations varied in the range of 102 to 196 nm and -9.4 to -13.8 mV, respectively. The lowest CMC values were calculated for 5:5 and 7:3 combinations (16.33 and 17.89 µM, respectively). The drug release rate from different formulations were very slow and only 30% of the drug was released during 72 h. Cytotoxicity assay demonstrated increased cytotoxic activity of PTX-loaded mixed micelles compared to the free drug. The in vitro deposition data indicated that spray drying of PTX-loaded micelles with lactose resulted in the production of inhalable powders with the high fine particle fraction (60%). Conclusion: These results demonstrate that this novel PTX-loaded micelles embedded in dry powder inhalation aerosol platform has a great potential to be used in lung cancer treatment.

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Published

2018-08-27

How to Cite

Rezazadeh, M., Davatsaz, Z., Emami, J., Hasanzadeh, F., & Jahanian-Najafabadi, A. (2018). Preparation and Characterization of Spray-Dried Inhalable Powders Containing Polymeric Micelles for Pulmonary Delivery of Paclitaxel in Lung Cancer. Journal of Pharmacy &Amp; Pharmaceutical Sciences, 21(1s), 200s–214s. https://doi.org/10.18433/jpps30048

Issue

Section

Pharmaceutical Sciences; Original Research Articles