Dry powder cationic lipopolymeric nanomicelle inhalation for targeted delivery of antitubercular drug to alveolar macrophage

Mithun Varghese Vadakkan,1 K Annapoorna,2 KC Sivakumar,3 Sathish Mundayoor,2 GS Vinod Kumar1 1Chemical Biology, 2Mycobacterium Research Group, 3Bioinformatics Facility, Rajiv Gandhi Centre for Biotechnology, Thiruvananthapuram, Kerala, India Abstract: Excipients having self-assembling properties are...

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Autores principales: Vadakkan MV, Annapoorna K, Sivakumar KC, Mundayoor S, Kumar GSV
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Publicado: Dove Medical Press 2013
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spelling oai:doaj.org-article:99d849c436d14de1bca156f03ed3e3c62021-12-02T02:01:52ZDry powder cationic lipopolymeric nanomicelle inhalation for targeted delivery of antitubercular drug to alveolar macrophage1176-91141178-2013https://doaj.org/article/99d849c436d14de1bca156f03ed3e3c62013-08-01T00:00:00Zhttp://www.dovepress.com/dry-powder-cationic-lipopolymeric-nanomicelle-inhalation-for-targeted--a13939https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Mithun Varghese Vadakkan,1 K Annapoorna,2 KC Sivakumar,3 Sathish Mundayoor,2 GS Vinod Kumar1 1Chemical Biology, 2Mycobacterium Research Group, 3Bioinformatics Facility, Rajiv Gandhi Centre for Biotechnology, Thiruvananthapuram, Kerala, India Abstract: Excipients having self-assembling properties are less explored in the field of dry powder inhalation (DPI) technology. An amphiphilic lipopolymer system was developed using stearic acid (SA) and branched polyethyleneimine (BPEI) (1800 Dalton), at different proportions by covalent conjugation. A molecular dynamic (MD) simulation tool was employed for predicting the carrier behavior in a polar in vivo condition. The structural characterization was carried out using nuclear magnetic resonance spectroscopy (NMR) and Fourier transform infrared (FTIR) spectroscopy. The physical nature of the lipopolymer was analyzed by differential scanning calorimetry. Determination of zeta potential and diameter of the micelles showed existence of cationic particles in the nano size range when a lower number of primary amino groups of BPEI was grafted with SA. The rifampicin (RIF)-loaded lipopolymer was also formulated further into spray-dried microparticles. Powder X-ray diffraction (PXRD) studies revealed that the RIF API (active pharmaceutical ingredient) exists as molecular dispersion in spray-dried microparticles. Topological analysis of the spray-dried nanomicelle was carried out using scanning electron microscopy (SEM). A large population of the drug-carrying particles were found to be under the inhalable size range (fine particle fraction 67.88% ± 3%). In vitro drug release kinetics from spray-dried nanomicelles were carried out at lung fluid pH. Keywords: molecular dynamics, dry powder inhalation, pulmonary tuberculosis, nanomicelle, lipopolymer, rifampicinVadakkan MVAnnapoorna KSivakumar KCMundayoor SKumar GSVDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2013, Iss default, Pp 2871-2885 (2013)
institution DOAJ
collection DOAJ
language EN
topic Medicine (General)
R5-920
spellingShingle Medicine (General)
R5-920
Vadakkan MV
Annapoorna K
Sivakumar KC
Mundayoor S
Kumar GSV
Dry powder cationic lipopolymeric nanomicelle inhalation for targeted delivery of antitubercular drug to alveolar macrophage
description Mithun Varghese Vadakkan,1 K Annapoorna,2 KC Sivakumar,3 Sathish Mundayoor,2 GS Vinod Kumar1 1Chemical Biology, 2Mycobacterium Research Group, 3Bioinformatics Facility, Rajiv Gandhi Centre for Biotechnology, Thiruvananthapuram, Kerala, India Abstract: Excipients having self-assembling properties are less explored in the field of dry powder inhalation (DPI) technology. An amphiphilic lipopolymer system was developed using stearic acid (SA) and branched polyethyleneimine (BPEI) (1800 Dalton), at different proportions by covalent conjugation. A molecular dynamic (MD) simulation tool was employed for predicting the carrier behavior in a polar in vivo condition. The structural characterization was carried out using nuclear magnetic resonance spectroscopy (NMR) and Fourier transform infrared (FTIR) spectroscopy. The physical nature of the lipopolymer was analyzed by differential scanning calorimetry. Determination of zeta potential and diameter of the micelles showed existence of cationic particles in the nano size range when a lower number of primary amino groups of BPEI was grafted with SA. The rifampicin (RIF)-loaded lipopolymer was also formulated further into spray-dried microparticles. Powder X-ray diffraction (PXRD) studies revealed that the RIF API (active pharmaceutical ingredient) exists as molecular dispersion in spray-dried microparticles. Topological analysis of the spray-dried nanomicelle was carried out using scanning electron microscopy (SEM). A large population of the drug-carrying particles were found to be under the inhalable size range (fine particle fraction 67.88% ± 3%). In vitro drug release kinetics from spray-dried nanomicelles were carried out at lung fluid pH. Keywords: molecular dynamics, dry powder inhalation, pulmonary tuberculosis, nanomicelle, lipopolymer, rifampicin
format article
author Vadakkan MV
Annapoorna K
Sivakumar KC
Mundayoor S
Kumar GSV
author_facet Vadakkan MV
Annapoorna K
Sivakumar KC
Mundayoor S
Kumar GSV
author_sort Vadakkan MV
title Dry powder cationic lipopolymeric nanomicelle inhalation for targeted delivery of antitubercular drug to alveolar macrophage
title_short Dry powder cationic lipopolymeric nanomicelle inhalation for targeted delivery of antitubercular drug to alveolar macrophage
title_full Dry powder cationic lipopolymeric nanomicelle inhalation for targeted delivery of antitubercular drug to alveolar macrophage
title_fullStr Dry powder cationic lipopolymeric nanomicelle inhalation for targeted delivery of antitubercular drug to alveolar macrophage
title_full_unstemmed Dry powder cationic lipopolymeric nanomicelle inhalation for targeted delivery of antitubercular drug to alveolar macrophage
title_sort dry powder cationic lipopolymeric nanomicelle inhalation for targeted delivery of antitubercular drug to alveolar macrophage
publisher Dove Medical Press
publishDate 2013
url https://doaj.org/article/99d849c436d14de1bca156f03ed3e3c6
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AT sivakumarkc drypowdercationiclipopolymericnanomicelleinhalationfortargeteddeliveryofantituberculardrugtoalveolarmacrophage
AT mundayoors drypowdercationiclipopolymericnanomicelleinhalationfortargeteddeliveryofantituberculardrugtoalveolarmacrophage
AT kumargsv drypowdercationiclipopolymericnanomicelleinhalationfortargeteddeliveryofantituberculardrugtoalveolarmacrophage
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