Login Register Cart 0
Generic placeholder image

Pharmaceutical Nanotechnology

Editor-in-Chief

ISSN (Print): 2211-7385
ISSN (Online): 2211-7393

Back
Journal Home About Journal Editorial Board Journal Insight Current Issue Volumes/Issues
Subscribe
Research Article

Eudragit RL100 Based Moxifloxacin Hydrochloride and Ketorolac Tromethamine Combination Nanoparticulate System for Ocular Drug Delivery

Author(s): Vedanti Salvi and Pravin Pawar *

Volume 8, Issue 2, 2020

Page: [133 - 147] Pages: 15

DOI: 10.2174/2211738508666200313140902

Price: $65

Abstract

Background: Bacterial conjunctivitis is a serious ocular infection if left untreated. It is caused by several species of bacteria like Pseudomonas, Staphylococcus and Mycobacterium.

Objective: The present investigation explores the development and characterization of moxifloxacin hydrochloride and ketorolac tromethamine combination loaded Eudragit RL 100 nanosuspension for ocular drug delivery in order to overcome the problems associated with conventional dosage forms.

Methods: The nanosuspension prepared by nanoprecipitation technique showed successful entrapment of both water-soluble drugs in the polymer matrix indicated by their % entrapment efficiencies.

Results: Formulations showed a mean particle size <200 nm with narrow size distribution and positive surface charge due to the presence of quaternary ammonium groups of Eudragit RL100. FTIR study revealed compatibility among the components, while a reduction in the crystallinity of formulation was observed in the PXRD study. The release of both the drugs was found to be sustained in nanosuspension as compared to commercial eyedrops. Ex vivo studies showed increased transcorneal permeation of drugs from nanosuspension, where approximately 2.5-fold and 2-fold increase in the permeation was observed for moxifloxacin hydrochloride and ketorolac tromethamine, respectively. The formulation was stable at 4°C and room temperature.

Conclusion: Due to their sustained release, positive surface charge and higher transcorneal permeation, this will be a promising ocular drug delivery.

Keywords: Drug combination, eudragit RL100, ketorolac tromethamine, moxifloxacin hydrochloride, nanosuspension, ocular drug delivery.

« Previous Next »
Graphical Abstract

[1]
Patel PB, Shastri DH, Shelat PK, Shukla AK. Ophthalmic drug delivery system: challenges and approaches. Sys Rev Pharm 2010; 1: 113-20.
[http://dx.doi.org/10.4103/0975-8453.75042]
[2]
Achouri D, Alhanout K, Piccerelle P, Andrieu V. Recent advances in ocular drug delivery. Drug Dev Ind Pharm 2013; 39(11): 1599-617.
[http://dx.doi.org/10.3109/03639045.2012.736515] [PMID: 23153114]
[3]
Weng Y, Liu J, Jin S, Guo W, Liang X, Hu Z. Nanotechnology-based strategies for treatment of ocular disease. Acta Pharm Sin B 2017; 7(3): 281-91.
[http://dx.doi.org/10.1016/j.apsb.2016.09.001] [PMID: 28540165]
[4]
Hutnik C, Mohammad-Shahi MH. Bacterial conjunctivitis. Clin Ophthalmol 2010; 4: 1451-7.
[http://dx.doi.org/10.2147/OPTH.S10162] [PMID: 21188158]
[5]
Mudgil M, Pawar PK. Preparation and in vitro/ex vivo evaluation of moxifloxacin-loaded PLGA nanosuspensions for ophthalmic applications. Sci Pharm 2013; 81(2): 591-606.
[http://dx.doi.org/10.3797/scipharm.1204-16] [PMID: 23833723]
[6]
Kaskoos RA. Investigation of moxifloxacin loaded chitosan-dextran nanoparticles for topical instillation into eye: In-vitro and ex-vivo evaluation. Int J Pharm Investig 2014; 4(4): 164-73.
[http://dx.doi.org/10.4103/2230-973X.143114] [PMID: 25426437]
[7]
Ibrahim HK, El-Leithy IS, Makky AA. Mucoadhesive nanoparticles as carrier systems for prolonged ocular delivery of gatifloxacin/prednisolone bitherapy. Mol Pharm 2010; 7(2): 576-85.
[http://dx.doi.org/10.1021/mp900279c] [PMID: 20163167]
[8]
Colin J. The role of NSAIDs in the management of postoperative ophthalmic inflammation. Drugs 2007; 67(9): 1291-308.
[http://dx.doi.org/10.2165/00003495-200767090-00004] [PMID: 17547472]
[9]
Fathalla ZM, Khaled KA, Hussein AK, Alany RG, Vangala A. Formulation and corneal permeation of ketorolac tromethamine-loaded chitosan nanoparticles. Drug Dev Ind Pharm 2016; 42(4): 514-24.
[http://dx.doi.org/10.3109/03639045.2015.1081236] [PMID: 26407208]
[10]
Prabhu P, Dubey A, Parth V, Ghate V. Investigation of hydrogel membranes containing combination of gentamicin and dexamethasone for ocular delivery. Int J Pharm Investig 2015; 5(4): 214-25.
[http://dx.doi.org/10.4103/2230-973X.167684] [PMID: 26682192]
[11]
Rossetti L, Bellucci R, Cillino S, et al. Efficacy and safety of combined diclofenac 0.1% and gentamicin 0.3% eyedrops after phacoemulsification. J Cataract Refract Surg 1997; 23(5): 745-9.
[http://dx.doi.org/10.1016/S0886-3350(97)80285-4] [PMID: 9278797]
[12]
Ermis SS, Aktepe OC, Inan UU, Ozturk F, Altindis M. Effect of topical dexamethasone and ciprofloxacin on bacterial flora of healthy conjunctiva. Eye (Lond) 2004; 18(3): 249-52.
[http://dx.doi.org/10.1038/sj.eye.6700631] [PMID: 15004572]
[13]
Pignatello R, Bucolo C, Puglisi G. Ocular tolerability of Eudragit RS100 and RL100 nanosuspensions as carriers for ophthalmic controlled drug delivery. J Pharm Sci 2002; 91(12): 2636-41.
[http://dx.doi.org/10.1002/jps.10227] [PMID: 12434408]
[14]
Costa P, Sousa Lobo JM. Modeling and comparison of dissolution profiles. Eur J Pharm Sci 2001; 13(2): 123-33.
[http://dx.doi.org/10.1016/S0928-0987(01)00095-1] [PMID: 11297896]
[15]
Pignatello R, Ricupero N, Bucolo C, Maugeri F, Maltese A, Puglisi G. Preparation and characterization of Eudragit Retard nanosuspensions for the ocular delivery of cloricromene. AAPS PharmSciTech 2006; 7(1): E192-8.
[http://dx.doi.org/10.1208/pt070127] [PMID: 28290042]
[16]
Pawar PK, Katara R, Majumdar DK. Design and evaluation of moxifloxacin hydrochloride ocular inserts. Acta Pharm 2012; 62(1): 93-104.
[http://dx.doi.org/10.2478/v10007-012-0002-5] [PMID: 22472452]
[17]
Morsi N, Ghorab D, Refai H, Teba H. Nanodispersion-loaded mucoadhesive polymeric inserts for prolonged treatment of post-operative ocular inflammation. J Microencapsul 2017; 34(3): 280-92.
[http://dx.doi.org/10.1080/02652048.2017.1321048] [PMID: 28420308]
[18]
Katara R, Majumdar DK. Eudragit RL 100-based nanoparticulate system of aceclofenac for ocular delivery. Colloids Surf B Biointerfaces 2013; 103: 455-62.
[http://dx.doi.org/10.1016/j.colsurfb.2012.10.056] [PMID: 23261566]
[19]
Mandal B, Alexander KS, Riga AT. Sulfacetamide loaded Eudragit® RL100 nanosuspension with potential for ocular delivery. J Pharm Pharm Sci 2010; 13(4): 510-23.
[http://dx.doi.org/10.18433/J3SW2T] [PMID: 21486528]
[20]
Yoshinari T, Forbes RT, York P, Kawashima Y. Moisture induced polymorphic transition of mannitol and its morphological transformation. Int J Pharm 2002; 247(1-2): 69-77.
[http://dx.doi.org/10.1016/S0378-5173(02)00380-0] [PMID: 12429486]

Rights & Permissions Print Cite
Article Metrics
13
1
© 2024 Bentham Science Publishers | Privacy Policy