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Drug Res (Stuttg) 2017; 67(06): 343-348
DOI: 10.1055/s-0043-102404
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

Development, In Vitro Characterization, Antitumor and Aerosol Performance Evaluation of Respirable Prepared by Self-nanoemulsification Method

Neda Naseri
1   Department of Medical Nanotechnology, School of Advanced Technologies in Medicine (SATiM), Tehran University of Medical Sciences, Tehran, Iran
,
Parvin Zakeri-Milani
2   Liver and Gastrointestinal Diseases Research Center and Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran
,
Hamed Hamishehkar
3   Drug Applied Research Center and Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran
,
Younes Pilehvar-Soltanahmadi
3   Drug Applied Research Center and Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran
,
Hadi Valizadeh
3   Drug Applied Research Center and Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran
› Author Affiliations
Further Information

Publication History

received 12 August 2016

accepted 20 January 2017

Publication Date:
13 March 2017 (online)

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Abstract

Poor water solubility and low oral bioavailability limit the clinical application of Erlotinib as an anticancer. For this purpose, we encapsulated erlotinib in the solid lipid nanoparticles (SLN) and designed a spray-dried dry powder inhalable (DPI) formulation. Erlotinib-loaded SLNs were prepared using self-nanoemulsifying and characterized for physicochemical properties. Pulmonary deposition of spray-dried DPI formulation was performed using Next Generation Impactor. The particle size and zeta potential of Erlotinib-loaded SLNs were 300 to 800 nm and −18 to −32 mV, respectively. High drug entrapment efficiency in the narrow range of 80–85% was achieved. Cytotoxicity results indicated that cell growth inhibition of free drug and drug loaded nanoparticles is dose- and time-dependent. Inhalable dry powders prepared from drug-loaded SLNs were found to have a fine particle fraction in the range of 6.92±0.99 –11.24±2.4%, mean mass aerodynamic diameter in the range of 4.52±0.1 to 6.67±0.5 µm. The findings revealed that the proposed inhalable dry powder formulation loaded with erlotinib SLN has potential in lung cancer therapy through pulmonary route.

Key word

drug delivery - bioavailability - anticancer drugs
 

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