J Pharm Bioallied Sci. 2012 Oct;4(4):333-40. doi: 10.4103/0975-7406.103274.

Formulation and optimization of nano-sized ethosomes for enhanced transdermal delivery of cromolyn sodium.

Journal of pharmacy & bioallied sciences

R Rakesh, K R Anoop

PMID: 23248569 PMCID: PMC3523531 DOI: 10.4103/0975-7406.103274

Abstract

AIM: The current study was aimed to investigate the feasibility of transdermal delivery of cromolyn sodium using a novel lipid vesicular carrier, ethosomes.

MATERIALS AND METHODS: Ethosomes of cromolyn sodium was prepared, optimized, and characterized for vesicle shape, vesicle size and size distribution, zeta potential, entrapment efficiency, in vitro drug release, in vitro skin permeation, in vitro skin deposition and vesicle stability. Histological examination of porcine ear skin treated with optimized ethosomal formulation was performed to study the change of skin morphologies.

RESULTS: The optimized cromolyn sodium ethosomes showed reasonable entrapment efficiency (49.88±1.84%), optimum nanometric size range (133.8 ± 7.5 nm), and high zeta potential (-69.82 ± 1.2 mV). In vitro drug release studies of optimized ethosomal formulation through cellophane membrane showed an enhanced and sustained delivery of drug compared to conventional liposomes, hydroethanolic, (45% v/v) and phosphate buffer saline PBS pH 7.4 drug solutions. The optimized ethosomal formulation showed significantly-enhanced transdermal flux (18.49 ± 0.08 mg/cm(2)/h) across porcine ear skin as compared to liposome (1.80 ± 0.12 mg/cm(2)/h), hydroethanolic drug solution (4.45 ± 0.71 mg/cm(2)/h), and PBS pH 7.4 drug solution (1.18 ± 0.35 mg/cm(2)/h). Moreover, ethosomal formulation showed better skin drug deposition (10.28 ± 0.67%) and shortest lag time (0.11 ± 0.09 h) for cromolyn sodium.

CONCLUSION: Our significant results suggest that ethosomes can be a promising tool for transdermal delivery of cromolyn sodium.

Keywords: Cromolyn sodium; ethosomes; liposomes; permeation enhancer

References

1. Biomaterials. 2000 Sep;21(18):1879-85 - PubMed
2. J Control Release. 2003 Dec 12;93(3):377-87 - PubMed
3. Nanomedicine. 2010 Aug;6(4):590-6 - PubMed
4. Int J Pharm. 2010 Mar 15;387(1-2):26-33 - PubMed
5. J Control Release. 2000 Apr 3;65(3):403-18 - PubMed
6. Acta Pol Pharm. 2010 May-Jun;67(3):217-23 - PubMed
7. Int J Pharm. 2005 Jul 14;298(1):1-12 - PubMed
8. Int J Pharm. 2008 Jun 24;358(1-2):128-36 - PubMed
9. Int J Pharm. 2003 Jan 30;251(1-2):49-56 - PubMed
10. AAPS PharmSciTech. 2007 Dec 21;8(4):E111 - PubMed
11. Int J Pharm. 2011 Apr 15;408(1-2):223-34 - PubMed
12. Biomaterials. 2001 Nov;22(22):3053-9 - PubMed
13. J Control Release. 2007 Nov 6;123(2):148-54 - PubMed
14. Oral Surg Oral Med Oral Pathol Oral Radiol Endod. 1999 Jun;87(6):700-5 - PubMed
15. Eur J Pharm Sci. 2008 Apr 23;33(4-5):424-33 - PubMed
16. J Control Release. 2005 Aug 18;106(1-2):99-110 - PubMed
17. Indian J Pharmacol. 2010 Jun;42(3):185-8 - PubMed
18. Int J Pharm. 2006 Sep 28;322(1-2):60-6 - PubMed
19. Ann Allergy Asthma Immunol. 1998 Nov;81(5):452-8 - PubMed
20. AAPS PharmSciTech. 2007 Dec 14;8(4):E107 - PubMed
21. J Control Release. 2004 Feb 10;94(2-3):365-79 - PubMed

Publication Types

• Journal Article