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Nanoemulsion Based Vehicle For Effective Ocular Delivery Of Moxifloxacin Using Experimental Design And Pharmacokinetic Study In Rabbits

Jigar Shah, Anroop B Nair, Shery Jacob, R. K. Patel, Hiral K Shah, Tamer M Shehata, M. Morsy
Published 2019 · Chemistry, Medicine

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Nanoemulsion is one of the potential drug delivery strategies used in topical ocular therapy. The purpose of this study was to design and optimize a nanoemulsion-based system to improve therapeutic efficacy of moxifloxacin in ophthalmic delivery. Moxifloxacin nanoemulsions were prepared by testing their solubility in oil, surfactants, and cosurfactants. A pseudoternary phase diagram was constructed by titration technique and nanoemulsions were obtained with four component mixtures of Tween 80, Soluphor® P, ethyl oleate and water. An experiment with simplex lattice design was conducted to assess the influence of formulation parameters in seven nanoemulsion formulations (MM1–MM7) containing moxifloxacin. Physicochemical characteristics and in vitro release of MM1–MM7 were examined and optimized formulation (MM3) was further evaluated for ex vivo permeation, antimicrobial activity, ocular irritation and stability. Drug pharmacokinetics in rabbit aqueous humor was assessed for MM3 and compared with conventional commercial eye drop formulation (control). MM3 exhibited complete drug release in 3 h by Higuchi diffusion controlled mechanism. Corneal steady state flux of MM3 (~32.01 µg/cm2/h) and control (~31.53 µg/cm2/h) were comparable. Ocular irritation study indicated good tolerance of MM3 and its safety for ophthalmic use. No significant changes were observed in the physicochemical properties of MM3 when stored in the refrigerator for 3 months. The greater aqueous humor concentration (Cmax; 555.73 ± 133.34 ng/mL) and delayed Tmax value (2 h) observed in MM3 suggest a reduced dosing frequency and increased therapeutic efficacy relative to control. The area under the aqueous humor concentration versus time curve (AUC0–8 h) of MM3 (1859.76 ± 424.51 ng·h/mL) was ~2 fold higher (p < 0.0005) than the control, suggesting a significant improvement in aqueous humor bioavailability. Our findings suggest that optimized nanoemulsion (MM3) enhanced the therapeutic effect of moxifloxacin and can therefore be used as a safe and effective delivery vehicle for ophthalmic therapy.
This paper references
10.1016/J.JCONREL.2005.11.020
W/O microemulsions for ocular delivery: evaluation of ocular irritation and precorneal retention.
R. Alany (2006)
10.1016/j.addr.2008.09.002
Polyoxyethylated nonionic surfactants and their applications in topical ocular drug delivery.
Jim Jiao (2008)
10.1016/j.ejpb.2015.02.019
Nanotherapies for the treatment of ocular diseases.
S. Reimondez-Troitiño (2015)
10.1055/s-0043-115124
Nanoemulsion: An Advanced Vehicle For Efficient Drug Delivery.
A. Ali (2017)
10.1111/j.1442-9071.2004.00914.x
New vehicle based on a microemulsion for topical ocular administration of dexamethasone
S. L. Fialho (2004)
10.1016/j.survophthal.2006.06.001
Ocular pharmacokinetics of moxifloxacin after topical treatment of animals and humans.
Joan-En Chang Lin (2006)
10.1208/s12249-009-9266-6
Development of an Ex Vivo Method for Evaluation of Precorneal Residence of Topical Ophthalmic Formulations
Q. Liu (2009)
10.5497/WJP.V2.I2.47
Ocular drug delivery systems: An overview.
Ashaben Patel (2013)
10.1007/BF00137947
The viscosity of human tears
J. Tiffany (2004)
10.1016/S0732-8893(01)00298-X
Comparative antimicrobial activity of gatifloxacin with ciprofloxacin and beta-lactams against gram-positive bacteria.
M. Bassetti (2001)
10.1002/JCCS.201000099
High-Performance Liquid Chromatography Assay for Moxifloxacin in Bulk, Pharmaceutical Formulations and Serum: Application to In-Vitro Metal Interactions
N. Sultana (2010)
Recent advances in non-ionic surfactant vesicles (niosomes): Selfassembly, fabrication, characterization, drug delivery applications and limitations
H. Abdelkader (2014)
10.3109/10717544.2014.943336
Liposomes in topical ophthalmic drug delivery: an update
R. Agarwal (2016)
Beyond the blink: Using in-situ gelling to optimize ophthalmic drug
J. N. Shah (2015)
10.3109/10717544.2014.948644
Development and evaluation of buccal films impregnated with selegiline-loaded nanospheres
Bandar E Aldhubiab (2016)
10.1016/j.ijpharm.2018.10.003
Prevention of rat liver fibrosis by selective targeting of hepatic stellate cells using hesperidin carriers
M. Morsy (2018)
10.1208/s12249-014-0156-1
Preclinical Formulations: Insight, Strategies, and Practical Considerations
S. M. Shah (2014)
10.1016/J.IJPHARM.2005.06.006
Phase behavior of the microemulsions and the stability of the chloramphenicol in the microemulsion-based ocular drug delivery system.
Feng-Feng Lv (2005)
10.1590/S1984-82502011000300003
Self-emulsifying therapeutic system: a potential approach for delivery of lipophilic drugs
J. Wadhwa (2011)
10.3109/10717544.2013.838077
Recent advances in non-ionic surfactant vesicles (niosomes): self-assembly, fabrication, characterization, drug delivery applications and limitations
H. Abdelkader (2014)
Ocular Drug Delivery
B. Gilger (2016)
10.1080/08982104.2016.1224897
Preparation and evaluation of niosome gel containing acyclovir for enhanced dermal deposition
Shery Jacob (2017)
10.1155/2013/826798
Microemulsion: New Insights into the Ocular Drug Delivery
R. R. Hegde (2013)
10.1016/j.ijpharm.2008.08.004
Novel microemulsion in situ electrolyte-triggered gelling system for ophthalmic delivery of lipophilic cyclosporine A: in vitro and in vivo results.
L. Gan (2009)
10.1002/ddr.21461
Dose translation between laboratory animals and human in preclinical and clinical phases of drug development
Anroop B Nair (2018)
10.1016/j.colsurfb.2015.10.045
Formulation and evaluation of nano based drug delivery system for the buccal delivery of acyclovir.
Bandar E Aldhubiab (2015)
10.3109/10717544.2012.704094
Enhanced oral bioavailability of calcium using bovine serum albumin microspheres
Anroop B Nair (2012)
Development and evaluation of buccal films impregnated with selegiline-loaded nanospheres
B. E. Al-Dhubiab (2016)
This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license
10.1021/ACS.IECR.8B04833
Phase Behavior and Microstructure of Symmetric Nonionic Microemulsions with Long-Chain n-Alkanes and Waxes
Kristina Schneider (2019)
10.1007/s12247-018-9312-6
Formulation and Evaluation of Chitosan-Based Buccal Bioadhesive Films of Zolmitriptan
R. Kumria (2018)
Beyond the blink : Using in - situ gelling to optimize ophthalmic drug delivery
J. N. Shah (2015)
10.1016/j.colsurfb.2010.07.029
Design and ocular tolerance of flurbiprofen loaded ultrasound-engineered NLC.
E. Gonzalez-Mira (2010)
10.2147/OPTH.S1666
Review of moxifloxacin hydrochloride ophthalmic solution in the treatment of bacterial eye infections
D. Miller (2008)
Identification of phases of various oil, surfactant/ co-surfactants and water system by ternary phase diagram.
H. K. Syed (2014)
10.1007/s40199-019-00242-x
Proniosomal gel for transdermal delivery of lornoxicam: optimization using factorial design and in vivo evaluation in rats
Hiral R. Shah (2019)
10.1007/s13346-016-0339-2
A comprehensive insight on ocular pharmacokinetics
Vibhuti Agrahari (2016)
10.1016/J.MOLLIQ.2014.12.043
The pseudo-ternary phase diagrams and properties of anionic–nonionic mixed surfactant reverse micellar systems
Ma Yujie (2015)



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10.1016/j.ijpharm.2020.119402
Nanoemulsion as a feasible and biocompatible carrier for ocular delivery of travoprost: improved pharmacokinetic/pharmacodynamic properties.
Ayman Ismail (2020)
10.1007/s13205-020-02262-w
Potential application of nanoemulsified garlic oil blend in mitigating the progression of type 2 diabetes-mediated nephropathy in Wistar rats
M. Yuvashree (2020)
10.3390/molecules24244566
Development of Asialoglycoprotein Receptor-Targeted Nanoparticles for Selective Delivery of Gemcitabine to Hepatocellular Carcinoma
Anroop B Nair (2019)
10.3390/pharmaceutics12050412
Pharmaceutical Particulates and Membranes for the Delivery of Drugs and Bioactive Molecules
D. B. Das (2020)
10.3390/pharmaceutics12070688
Surface Active Agents and Their Health-Promoting Properties: Molecules of Multifunctional Significance
I. Anestopoulos (2020)
10.3390/ma12244239
HPMC- and PLGA-Based Nanoparticles for the Mucoadhesive Delivery of Sitagliptin: Optimization and In Vivo Evaluation in Rats
Anroop B Nair (2019)
10.3390/pharmaceutics12090893
Development and Optimization of Naringenin-Loaded Chitosan-Coated Nanoemulsion for Topical Therapy in Wound Healing
Sabah H. Akrawi (2020)
10.3390/pharmaceutics11110609
Preparation and Evaluation of Atorvastatin-Loaded Nanoemulgel on Wound-Healing Efficacy
M. Morsy (2019)
10.1016/j.jconrel.2020.10.025
Therapeutic nanoemulsions in ophthalmic drug administration: Concept in formulations and characterization techniques for ocular drug delivery.
M. Singh (2020)
10.1016/j.ijpharm.2019.118991
Iontophoresis enhances voriconazole antifungal potency and corneal penetration.
G. M. Gelfuso (2019)
10.33263/briac111.77547764
Thermosensitive Brinzolamide in situ Gel Nanoemulsions, in vitro and ex vivo Evaluation
Mohammad Mehdi Mahboobian (2020)
10.3390/app10155341
Vesicular Emulgel Based System for Transdermal Delivery of Insulin: Factorial Design and in Vivo Evaluation
Anroop B Nair (2020)
10.1080/10717544.2020.1797237
Development, optimization, and evaluation of PEGylated brucine-loaded PLGA nanoparticles
Heba S Elsewedy (2020)
10.3390/polym11101699
Gellan Gum-Based Hydrogel for the Transdermal Delivery of Nebivolol: Optimization and Evaluation
Anroop B Nair (2019)
10.1016/j.jddst.2019.101400
Development of thermosensitive in situ gel nanoemulsions for ocular delivery of acyclovir
Mohammad Mehdi Mahboobian (2020)
10.2174/1872211314666191224115211
Nano-Based Drug Delivery System: Recent Strategies for the Treatment of Ocular Disease and Future Perspective
Zufika Qamar (2019)
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