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Ligand Mediated Carbon Nanotubes Based

Delivery of an Anticancer Agent

Article in LATIN AMERICAN JOURNAL OF PHARMACY October 2017

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 Latin American Journal of Pharmacy Received: July 29, 2017
(formerly Acta Farmacutica Bonaerense) Revised version: August 30, 2017

Lat. Am. J. Pharm. 36 (10): 2081-91 (2017) Accepted: August 31, 2017

Ligand Mediated Carbon Nanotubes Based Delivery

of an Anticancer Agent

B. MANGLA 1, Kuldeep S. PATEL 1*, P. KUMAR 2 & Giriraj T. KULKARNI 1 *

Department of Pharmaceutics, Amity Institute of Pharmacy,

1

Amity University, Noida, Uttar Pradesh, India-201307

2 Department of Pharmaceutics, Advanced Institute of Pharmacy, Palwal, Haryana, India-121102

SUMMARY. The proposed work envisages the development of folate-conjugated irinotecan hydrochloride
loaded carbon nanotubes. These systems have the advantage of direct penetration to the cells and folate-
conjugation would further provide them with targeting ability. Rationale of selecting folate conjugated is
their selective localization in the vicinity of folate receptor and its easy amino conjugation to carbon nan-
otubes. Irinotecan hydrochloride was selected as model drug due to its aqueous solubility and high proba-
bility of drug loading in carbon nanotubes. Multi-walled carbon nanotubes were purified and functional-
ized with folic acid using 1-ethyl-3-(-3-dimethylaminopropyl) carbodiimide hydrochloride and N-Hydrox-
ysuccinimide. After functionalization, various characterization parameters like dispersion characteristics,
Fourier-transform infrared spectroscopy, elemental analysis, X-Ray diffraction, scanning electron micro-
scope analysis, particle size determination and zeta potential were performed. After conjugation of folic
acid with multi-walled carbon nanotubes, drug was loaded and then characterized for loading efficiency
and in vitro drug release. Sustained-release behavior was an important factor for drug delivery systems
and prepared carbon nanotubes depicted the same during in vitro drug release studies. The drug loading
efficiency of carboxylated multi-walled carbon nanotubes was higher than purified multi-walled carbon
nanotubesand folate conjugated. Multi-walled carbon nanotubes suggested comparatively less entrapment
of drug due to its high dispersity and steric hindrance. Thus, the folate-conjugated multi-walled carbon
nanotubes prepared in this experiment shows great potential as an advanced drug delivery system and
have tremendous useful properties not seen in any other delivery module.
RESUMEN. El trabajo propuesto prev el desarrollo de nanotubos de carbono cargados con clorhidrato de irino-
tecn conjugado con folato. Estos sistemas tienen la ventaja de la penetracin directa a las clulas y la conjuga-
cin de folato les proporcionara adems capacidad de direccionamiento. La razn de seleccionar el folato conju-
gado es su localizacin selectiva en las proximidades del receptor de folato y su fcil amino-conjugacin a los
nanotubos de carbono. El clorhidrato de irinotecn fue seleccionado como frmaco modelo debido a su solubili-
dad acuosa y alta probabilidad de carga de frmaco en los nanotubos de carbono. Los nanotubos de carbono de
paredes mltiples se purificaron y funcionalizaron con cido flico usando hidrocloruro de 1-etil-3-(-3-dimetila-
minopropil) carbodiimida y N-hidroxisuccinimida. Despus de la funcionalizacin, se realizaron diversos par-
metros de caracterizacin como caractersticas de dispersin, espectroscopa infrarroja por transformada de Fou-
rier, anlisis elemental, difraccin de rayos X, anlisis con microscopio electrnico de barrido, determinacin del
tamao de partcula y potencial zeta. Despus de la conjugacin de cido flico con nanotubos de carbono de
mltiples paredes, el frmaco se carg y luego se caracteriz por la eficiencia de carga y la liberacin in vitro del
frmaco. El comportamiento de liberacin sostenida fue un factor importante para los sistemas de administracin
de frmacos y los nanotubos de carbono preparados representaron lo mismo durante los estudios de liberacin de
frmaco in vitro. La eficacia de carga de frmacos de los nanotubos de carbono con paredes mltiples carboxila-
das fue mayor que la de los nanotubos de carbono de paredes mltiples purificados y el folato conjugado de na-
notubos de carbono de paredes mltiples comparativamente menos atrapamiento de frmaco, debido a su alta
dispersidad e impedimento estrico. De este modo, los nanotubos de carbono de mltiples paredes conjugados
con folato preparados en este experimento muestran un gran potencial como un sistema avanzado de suministro
de frmacos y tienen enormes propiedades tiles que no se ven en ningn otro modo de administracin.

KEY WORDS: anti-cancer drugs, carbon nanotubes, folic acid, multi-walled carbon nanotubes.
* Author to whom correspondence should be addressed. E-mail: kuldeeppharmacy@gmail.com

ISSN 0326 2383 (printed ed.)

ISSN 2362-3853 (on line ed.) 2081

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