Formulation of Losartan Nanoparticles with Chitosan as a Carrier

  • AKHMAD KHARIS NUGROHO UNIVERSITAS GADJAH MADA
  • NURI ARI EFIANA UNIVERSITAS GADJAH MADA
  • RONNY MARTIEN UNIVERSITAS GADJAH MADA

Abstract

Nanoparticle formulation is important for systemic drug delivery via several routes. This research was aimed to establish optimal formation of chitosan nanoparticle formulation with losartan, an antihypertension known as an angiotensin II receptor antagonist. Ionic gelation method was used. Formulation was established in 2 steps. Firstly, determination of the best losartan and chitosan concentrations which can produce physically stable nanoparticles without precipitation, at room temperature within 25 days. Secondly, optimization of the process by factorial design method of two factors, including pH (4.0 and 5.0) and the stirring rate (350 and 700 rpm), with the loading capacity of the nanoparticle as the observed response. The obtained nanoparticles were evaluated further for its particle size and zeta potential. The physichal stability tests indicated that two nanoparticle formulations containing losartan-chitosan of (14 mg% : 35 mg%), and losartan-chitosan of (21 mg% : 35 mg%) were stable. The factorial design studies suggested that pH 4 and the stirring rate of 350 rpm were the optimal conditions which produced the highest loading capacity (47,7%). The particle size and zeta potential of the stable nanoparticle were 290.3±52.6 nm and +50.8 ±4.8 mV respectively.

References

1. Diez J. Review of the molecular pharmacology of losartan and its possible to stroke prevention in patients with hypertension. Clinic Therap. 2006.28(6):832-48.
2. Vijayan V, Sumanth MH, Suman L, VinayT, Srinivasrao D, Kumar KJ. Development and physiochemical, In vitro evaluation of antihypertensive transdermal patches. J Pharm Sci & Res. 2010.2(3):171-7.
3. Hafner A, Lovrić J, Pepić I, Filipović-Grčić J. Lecithin/chitosan nanoparticles for transdermal delivery of melatonin. J Microencapsul. 2011.28(8):807–15.
4. Slütter B, Bal S, Keijzer C, Mallants R, Hagenaars N, Que I, et al. Nasal vaccination with N-trimethyl chitosan and PLGA based nanoparticles: nanoparticle characteristics determine quality and strength of the antibody response in mice against the encapsulated antigen. Vaccine. 2010.28(38):6282–91.
5. Sung JC, Padilla DJ, Garcia-Contreras L, Verberkmoes JL, Durbin D, Peloquin CA, et al. Formulation and pharmacokinetics of self-assembled rifampicin nanoparticle systems for pulmonary delivery. Pharm. Res. 2009.26(8):1847–55
6. Majeti NV, Kumar R. A review of chitin and chitosan applications. React Funct Polym. 2000.46:1–27.
7. Tiyaboonchai W. Chitosan nanoparticles: A promising system for drug delivery. Naresuan Univ J. 2003.11(3):51-66.
8. Patel JK, Jivani NP. Chitosan based nanoparticles in drug delivery. Int Phar Sci Nanotech. 2009.2(2):517-22.
9. Racovita S, Vasiliu S, Popa M, Luca C. Polysaccharides based on micro- and nanoparticles obtained by ionic gelation and their application as drug delivery systems review. Revue Roumaine de Chimie. 2009.54(9):709-18.
10. Mohanraj VJ, Chen Y. Nanoparticles – A Review. Trop. J Pharm Research. 2006.5(1):561-73.
11. Seburg RA, Ballard, JM, Hwang TL, Sullivan CM. Photosensitized degradation of losartan potassium in an extemporaneous suspension formulation. J Pharm Biomed Anal. 2006.42(4):411–22.
12. Jang K and Lee G. Stability of chitosan nanoparticles for L-ascorbic acid during heat treatment in aqueous solution. J Agric Food Chem. 2008.56:1936-41.
13. Saha P, Goyal AK, Rath G. Formulation and evaluation of chitosan-based ampicillin trihydrate nanoparticles. Trop J Pharm Research. 2010.9(5):483-8.
14. Binarjo A. Pengaruh kadar obat, kadar propilen glikol dan lama praperlakuan dengan asam oleat terhadap transpor transdermal losartan in vitro [tesis]. Yogyakarta: Fakultas Farmasi Universitas Gadjah Mada; 2010.
15. Campos AM, Sanchez A, Alonso MJ. Chitosan nanoparticles: A new vehicle for the improvement of the delivery of drugs to the ocular surface. Application to cyclosporin A. Int J Pharm. 2001.224:159–68.
16. Selvaraj S, Saravanakumar N, Karthikeyan J, Evangeline D, Rajendran L. Acyclovir loaded chitosan nanoparticles for ocular delivery. Der Pharmacia Lettre. 2010.2(3):420-31.
17. Sinko PJ. Martin’s physical pharmacy and pharmaceutical sciences. Philadelphia: Lippincott Williams & Wilkins; 2006. 187–229.
18. Manmode AS, Sakarkar DM, Mahajan NM. Nanoparticles-tremendous therapeutic potential: A review. Int J PharmTech Res. 2009.1(4):1020-7.
19. Dustgani A, Farahani EV, Imani M. Preparation of chitosan nanoparticles loaded by dexamethasone sodium phosphate. Iranian J Pharm Sci. 2008.4(2):111-14.
Published
2013-04-30
How to Cite
NUGROHO, AKHMAD KHARIS; EFIANA, NURI ARI; MARTIEN, RONNY. Formulation of Losartan Nanoparticles with Chitosan as a Carrier. JURNAL ILMU KEFARMASIAN INDONESIA, [S.l.], v. 11, n. 1, p. 7-12, apr. 2013. ISSN 2614-6495. Available at: <http://jifi.farmasi.univpancasila.ac.id/index.php/jifi/article/view/225>. Date accessed: 19 dec. 2024.
Section
Articles