- Email: [email protected]
Modification of ChPL (chitosan protein–lipid) nanoparticles for in vitro release of rifampicin (RIF)
International Journal of Mycobacteriology
H O S T E D BY
4 (2015) 16
Available at www.sciencedirect.com
ScienceDirect journal homepage: www.elsevier.com/locate/IJMYCO
Modification of ChPL (chitosan protein–lipid) nanoparticles for in vitro release of rifampicin (RIF) Poopak Farnia a, Jalaledin Ghanavi Ali Akbar Velayati c
a,*
, Saeed Mollaei b, Afshin Bahrami a,
a
Experimental Medicine and Tissue Engineering Center, National Research Institute of Tuberculosis and Lung Disease (NRITLD), Shahid Beheshti University of Medical Sciences, Tehran, Iran b Medicinal plant and drug Research Institute, Shahid Beheshti University, Tehran, Iran c Mycobacteriology Research Center, National Research Institute of Tuberculosis and Lung Disease (NRITLD), Shahid Beheshti University of Medical Sciences, Tehran, Iran
A R T I C L E I N F O
A B S T R A C T
Article history:
During recent years, the implication of nanoparticles (NPs) as drug delivery systems has
Received 19 November 2014
gained much scientific attention. As drugs do not deliver themselves, a nanoparticle can
Accepted 23 November 2014
act by optimizing drug delivery in the right place, at the right time and at the right dosage.
Available online 6 January 2015
In previous years, this research successfully developed and evaluated the ChPL-NPs nanoparticles (chitosan protein–lipid) [US patent pending 20140370500]. In the present
Keywords:
investigation, rifampicin (RIF) ChPL-NPs nanoparticles were designed and developed.
ChPL-NPs
Consequently, the in vitro release of RIF ChPL-NPs nanoparticles was investigated.
Nanoparticles
Material and methods: Briefly, chitosan powder (90 KD and 90% degree of deacetylation) was
RIF
dissolved (1% acetic-acid) and mixed with gelatin (3%). Then, the lipid and rifampin in ether
Antimycobacterial activity
was precipitated by rotary vacuum evaporator. Under high speed homogenizer (12,000 rpm), both solutions (chitosan–gelatin & rifampin–lipid) were mixed [US patent pending 20140370500]. The obtained RIF ChPL-NPs were put into a dialysis bag with cut-off 14 KD in phosphate buffer solution (pH = 7.4). The release of RIF was obtained by reverse phase HPLC using C18 (250 · 4.6 mm, 5 lm) column. The mobile phase consisted of 50:50 v/v acetonitrile and 10 mm potassium dihydrogen phosphate (pH = 3.2) and flow rate 1 ml/min. The column temp was maintained at 25 C with UV detection at 335 nm. Results and conclusions: The average size of RIF ChPL-NPs was about 50–250 nm. The release of RIF from the dialysis bag started after 30 min which was 2400 ng/ml; after 16 h the release of RIF was 15,000 ng/ml; and at 40 h the concentration reached to 19,600 ng/ml. Therefore, these results showed a slow release of RIF from ChPL-NPs. Basically, the intensity of the surface charges in nanoparticle is important as it determines their interaction with bioactive compound. In RIF ChPL-NPs, lipid had negative charges, whereas chitosan and gelatin had positive charges. The electrostatic interaction between oppositely charged ions would ultimately cause an effective system drug delivery. RIF ChPL-NPs is not only suitable for intravenous administration, but it can be used as an inhalation aerosol, because this nanoparticle has a capacity to adhere to mucosal surfaces and transiently open the tight junction. 2015 Asian-African Society for Mycobacteriology. Published by Elsevier Ltd. All rights reserved.
* Corresponding author at: Experimental Medicine and Tissue Engineering Center, National Research Institute of Tuberculosis and Lung Disease (NRITLD), Shahid Beheshti University of Medical Sciences, P.O. 19575/154, Tehran 19556, Iran. E-mail address: [email protected] (J. Ghanavi). http://dx.doi.org/10.1016/j.ijmyco.2014.11.038 2212-5531/ 2015 Asian-African Society for Mycobacteriology. Published by Elsevier Ltd. All rights reserved.
H O S T E D BY
4 (2015) 16
Available at www.sciencedirect.com
ScienceDirect journal homepage: www.elsevier.com/locate/IJMYCO
Modification of ChPL (chitosan protein–lipid) nanoparticles for in vitro release of rifampicin (RIF) Poopak Farnia a, Jalaledin Ghanavi Ali Akbar Velayati c
a,*
, Saeed Mollaei b, Afshin Bahrami a,
a
Experimental Medicine and Tissue Engineering Center, National Research Institute of Tuberculosis and Lung Disease (NRITLD), Shahid Beheshti University of Medical Sciences, Tehran, Iran b Medicinal plant and drug Research Institute, Shahid Beheshti University, Tehran, Iran c Mycobacteriology Research Center, National Research Institute of Tuberculosis and Lung Disease (NRITLD), Shahid Beheshti University of Medical Sciences, Tehran, Iran
A R T I C L E I N F O
A B S T R A C T
Article history:
During recent years, the implication of nanoparticles (NPs) as drug delivery systems has
Received 19 November 2014
gained much scientific attention. As drugs do not deliver themselves, a nanoparticle can
Accepted 23 November 2014
act by optimizing drug delivery in the right place, at the right time and at the right dosage.
Available online 6 January 2015
In previous years, this research successfully developed and evaluated the ChPL-NPs nanoparticles (chitosan protein–lipid) [US patent pending 20140370500]. In the present
Keywords:
investigation, rifampicin (RIF) ChPL-NPs nanoparticles were designed and developed.
ChPL-NPs
Consequently, the in vitro release of RIF ChPL-NPs nanoparticles was investigated.
Nanoparticles
Material and methods: Briefly, chitosan powder (90 KD and 90% degree of deacetylation) was
RIF
dissolved (1% acetic-acid) and mixed with gelatin (3%). Then, the lipid and rifampin in ether
Antimycobacterial activity
was precipitated by rotary vacuum evaporator. Under high speed homogenizer (12,000 rpm), both solutions (chitosan–gelatin & rifampin–lipid) were mixed [US patent pending 20140370500]. The obtained RIF ChPL-NPs were put into a dialysis bag with cut-off 14 KD in phosphate buffer solution (pH = 7.4). The release of RIF was obtained by reverse phase HPLC using C18 (250 · 4.6 mm, 5 lm) column. The mobile phase consisted of 50:50 v/v acetonitrile and 10 mm potassium dihydrogen phosphate (pH = 3.2) and flow rate 1 ml/min. The column temp was maintained at 25 C with UV detection at 335 nm. Results and conclusions: The average size of RIF ChPL-NPs was about 50–250 nm. The release of RIF from the dialysis bag started after 30 min which was 2400 ng/ml; after 16 h the release of RIF was 15,000 ng/ml; and at 40 h the concentration reached to 19,600 ng/ml. Therefore, these results showed a slow release of RIF from ChPL-NPs. Basically, the intensity of the surface charges in nanoparticle is important as it determines their interaction with bioactive compound. In RIF ChPL-NPs, lipid had negative charges, whereas chitosan and gelatin had positive charges. The electrostatic interaction between oppositely charged ions would ultimately cause an effective system drug delivery. RIF ChPL-NPs is not only suitable for intravenous administration, but it can be used as an inhalation aerosol, because this nanoparticle has a capacity to adhere to mucosal surfaces and transiently open the tight junction. 2015 Asian-African Society for Mycobacteriology. Published by Elsevier Ltd. All rights reserved.
* Corresponding author at: Experimental Medicine and Tissue Engineering Center, National Research Institute of Tuberculosis and Lung Disease (NRITLD), Shahid Beheshti University of Medical Sciences, P.O. 19575/154, Tehran 19556, Iran. E-mail address: [email protected] (J. Ghanavi). http://dx.doi.org/10.1016/j.ijmyco.2014.11.038 2212-5531/ 2015 Asian-African Society for Mycobacteriology. Published by Elsevier Ltd. All rights reserved.