Online citations, reference lists, and bibliographies.
← Back to Search

The Role Of Surface Active Agents In Ophthalmic Drug Delivery: A Comprehensive Review.

Shaimaa S Ibrahim
Published 2019 · Medicine, Chemistry

Cite This
Download PDF
Analyze on Scholarcy
Share
With the significant advances made in nanotechnology, research efforts focused on developing novel drug delivery platforms that can overcome the multitude of challenges encountered in ophthalmic drug delivery. Surface active agents (SAAs) have been extensively used for the formulation of many of the dosage forms targeting ocular tissues. Novel ophthalmic carriers utilizing SAAs were broadly classified into particulate, vesicular, and controlled release drug delivery systems. Depending on their physicochemical properties, SAAs can perform a variety of roles ranging from wetting agents, emulsifiers, stabilizers, charge inducers, solubilizers, antimicrobial agents, corneal permeation enhancers, and gelling agents. Nevertheless, their use is limited by their potential toxicity and possible interactions with other formulation ingredients. This review provides a comprehensive analysis of the different functional roles of SAAs in novel ophthalmic drug delivery platforms, their mechanism of action, and limitations that need to be considered during formulation to maximize their potential benefit. Understanding the mechanisms by which they perform their different roles and the possible interactions between SAAs and other formulation ingredients can help orientate the choice of formulators toward the SAA most suitable for the intended ocular application at a concentration that is both safe and effective.
This paper references
10.1016/J.JFO.2017.01.004
Surveillance, hygiène et entretien des lentilles de contact☆
L. Bloise (2017)
10.1016/j.sjopt.2014.06.006
Balancing antimicrobial efficacy and toxicity of currently available topical ophthalmic preservatives.
E. Tu (2014)
10.4155/tde-2016-0076
Development of microemulsions for ocular delivery.
Nivedita Gautam (2017)
10.1155/2014/263604
Nonionic Surfactant Vesicles in Ocular Delivery: Innovative Approaches and Perspectives
R. K. Sahoo (2014)
10.1016/0927-7765(93)01111-4
Surface properties of mixed phospholipid—stearylamine monolayers and their interaction with a non-ionic surfactant (poloxamer)
D. Korner (1994)
10.1021/JS950474+
Comparative in vitro evaluation of several colloidal systems, nanoparticles, nanocapsules, and nanoemulsions, as ocular drug carriers.
P. Calvo (1996)
10.1016/j.ijpharm.2012.12.049
Promising ion-sensitive in situ ocular nanoemulsion gels of terbinafine hydrochloride: design, in vitro characterization and in vivo estimation of the ocular irritation and drug pharmacokinetics in the aqueous humor of rabbits.
S. Tayel (2013)
10.1016/j.ejps.2017.03.001
Synthetic nanocarriers for the delivery of polynucleotides to the eye
S. Saraiva (2017)
Injectable microspheres with controlled drug release for glaucoma filtering surgery.
H. Kimura (1992)
10.1081/DDC-120001491
Ophthalmic Vehicles Containing Polymer-Solubilized Tropicamide: “In Vitro/In Vivo” Evaluation
C. Carmignani (2002)
10.3109/08982108909036000
Adhesion of Positively Charged Liposomes to Mucosal Tissues
L. S. Guo (1989)
10.1208/s12249-008-9121-1
Effect of Charged and Non-ionic Membrane Additives on Physicochemical Properties and Stability of Niosomes
V. Junyaprasert (2008)
10.1016/j.ijpharm.2011.02.051
Nanosuspension for improving the bioavailability of a poorly soluble drug and screening of stabilizing agents to inhibit crystal growth.
Indrajit K. Ghosh (2011)
10.1016/j.addr.2008.09.002
Polyoxyethylated nonionic surfactants and their applications in topical ocular drug delivery.
Jim Jiao (2008)
10.1080/03639040801926030
Ocular Poloxamer-Based Ciprofloxacin Hydrochloride In Situ Forming Gels
M. Mansour (2008)
10.4172/2155-9570.1000408
A Novel Pilocarpine Microemulsion as an Ocular Delivery System: In Vitro and In Vivo Studies
Iskender Ince (2015)
10.3109/02713681003760168
Feasibility of Lipid Nanoparticles for Ocular Delivery of Anti-Inflammatory Drugs
E. Souto (2010)
10.1081/DDC-120002997
Penetration Enhancers and Ocular Bioadhesives: Two New Avenues for Ophthalmic Drug Delivery
I. P. Kaur (2002)
10.1208/s12249-009-9373-4
Ciprofloxacin as Ocular Liposomal Hydrogel
K. Hosny (2009)
10.1016/J.IJPHARM.2007.11.013
The delivery and antinociceptive effects of morphine and its ester prodrugs from lipid emulsions.
J. Wang (2008)
10.1097/ICO.0000000000000825
Voriconazole-Loaded Nanostructured Lipid Carriers for Ocular Drug Delivery
L. M. Andrade (2016)
Biodegradable microspheres containing adriamycin in the treatment of proliferative vitreoretinopathy.
T. Moritera (1992)
10.1016/j.ijpharm.2011.04.027
Spanlastics--a novel nanovesicular carrier system for ocular delivery.
S. Kakkar (2011)
10.1016/S1461-5347(99)00141-8
Top ten considerations in the development of parenteral emulsions.
Floyd (1999)
10.1080/09273948.2017.1333622
Ocular Self-Microemulsifying Drug Delivery System of Prednisolone Improves Therapeutic Effectiveness in the Treatment of Experimental Uveitis
R. Tiwari (2019)
10.1016/J.IJPHARM.2007.03.011
Nanosuspension as an ophthalmic delivery system for certain glucocorticoid drugs.
M. Kassem (2007)
10.1089/jop.2013.0157
Aqueous nanomicellar formulation for topical delivery of biotinylated lipid prodrug of acyclovir: formulation development and ocular biocompatibility.
A. D. Vadlapudi (2014)
10.1155/2014/490595
Design and Evaluation of Voriconazole Eye Drops for the Treatment of Fungal Keratitis
S. Malhotra (2014)
10.3390/scipharm86020016
Ocular Delivery System for Propranolol Hydrochloride Based on Nanostructured Lipid Carrier
Behzad Sharif Makhmal Zadeh (2018)
10.15415/JPTRM.2013.11004
Surfactants: Pharmaceutical and Medicinal Aspects
B. S. Sekhon (2013)
10.2174/1877912311202020082
Novel Nanomicellar Formulation Approaches for Anterior and Posterior Segment Ocular Drug Delivery.
K. Cholkar (2012)
NANOTECHNOLOGY: A NEW APPROACH FOR OCULAR DRUG DELIVERY SYSTEM
Meetali Mudgil (2012)
10.1021/acsami.5b12688
Selective Antimicrobial Activities and Action Mechanism of Micelles Self-Assembled by Cationic Oligomeric Surfactants.
C. Zhou (2016)
10.1208/s12249-009-9257-7
Investigation on Processing Variables for the Preparation of Fluconazole-Loaded Ethyl Cellulose Microspheres by Modified Multiple Emulsion Technique
Sabyasachi Maiti (2009)
10.3389/fphar.2018.00285
Innovative Nanoparticles Enhance N-Palmitoylethanolamide Intraocular Delivery
C. Puglia (2018)
10.1023/A:1013671819604
Cyclosporine A Formulation Affects Its Ocular Distribution in Rabbits
M. Kuwano (2004)
10.1016/0378-5173(96)04663-7
Evaluation of ocular permeation enhancers: In vitro effects on corneal transport of four β-blockers, and in vitro/in vivo toxic activity
M. Saettone (1996)
10.3109/10717544.2014.893381
Engineering of polymer–surfactant nanoparticles of doxycycline hydrochloride for ocular drug delivery
V. Pokharkar (2015)
10.1517/17425247.2014.935338
Advances in ocular drug delivery: emphasis on the posterior segment
Jennifer J. Kang-Mieler (2014)
10.1016/j.ejpb.2017.03.006
Cyclosporine A delivery to the eye: A comprehensive review of academic and industrial efforts
F. Lallemand (2017)
10.1007/s11095-009-0042-9
New Techniques for Drug Delivery to the Posterior Eye Segment
E. Eljarrat-Binstock (2009)
10.1016/S0887-2333(03)00052-3
Ocular toxicity of some corneal penetration enhancers evaluated by electrophysiology measurements on isolated rabbit corneas.
P. Chetoni (2003)
10.7150/thno.22711
Recent Advances in the Application of Vitamin E TPGS for Drug Delivery
Conglian Yang (2018)
10.1038/aps.2010.98
Novel vehicle based on cubosomes for ophthalmic delivery of flurbiprofen with low irritancy and high bioavailability
S. Han (2010)
10.1016/S0378-5173(00)00540-8
Application of in vivo confocal microscopy to the objective evaluation of ocular irritation induced by surfactants.
P. Furrer (2000)
10.1080/15569520600860587
Prediction of Eye Irritation Potential of Surfactant-Based Rinse-Off Personal Care Formulations by the Bovine Corneal Opacity and Permeability (BCOP) Assay
K. C. Cater (2006)
10.2174/1872211308666140926112000
Recent patents on ophthalmic nanoformulations and therapeutic implications.
Ann-Marie Ako-Adounvo (2014)
10.1016/j.colsurfb.2008.11.034
Comparative effects of different cosurfactants on sterile prednisolone acetate ocular submicron emulsions stability and release.
Shaimaa S Ibrahim (2009)
10.3109/10717544.2014.923065
Colloidal drug delivery system: amplify the ocular delivery
Ameeduzzafar (2016)
10.1016/j.drudis.2007.10.021
Nanotechnology in ocular drug delivery.
S. Sahoo (2008)
10.1016/j.colsurfb.2012.08.021
Further investigation of nanostructured lipid carriers as an ocular delivery system: in vivo transcorneal mechanism and in vitro release study.
Bao-Cheng Tian (2013)
10.1016/j.ijpharm.2017.07.065
Non-invasive strategies for targeting the posterior segment of eye.
Asadullah Madni (2017)
10.1208/aapsj0903044
Preparation and ocular pharmacokinetics of ganciclovir liposomes
Y. Shen (2008)
Ocular delivery of cyclosporin A. II. Effect of submicron emulsion's surface charge on ocular distribution of topical cyclosporin A
M. Abdulrazik (2001)
10.1016/j.jsps.2013.07.003
Design of liposomal colloidal systems for ocular delivery of ciprofloxacin.
E. Taha (2014)
10.1155/2013/348186
Pharmacosomes: An Emerging Novel Vesicular Drug Delivery System for Poorly Soluble Synthetic and Herbal Drugs
Archana Pandita (2013)
10.2147/IJN.S51186
Self-aggregated nanoparticles based on amphiphilic poly(lactic acid)-grafted-chitosan copolymer for ocular delivery of amphotericin B
W. Zhou (2013)
10.1016/J.IJPHARM.2003.11.032
Micellar solutions of triblock copolymer surfactants with pilocarpine.
I. Pepić (2004)
10.1016/j.biomaterials.2008.10.032
Surfactant-laden soft contact lenses for extended delivery of ophthalmic drugs.
Yash Kapoor (2009)
10.1211/0022357991772664
Characterization and In‐vivo Ocular Absorption of Liposome‐encapsulated Acyclovir
M. Fresta (1999)
10.1016/S0378-5173(99)00265-3
Preparation and evaluation of liposomal formulations of tropicamide for ocular delivery.
M. Nagarsenker (1999)
10.1080/21645515.2015.1046660
Impact of formulation and particle size on stability and immunogenicity of oil-in-water emulsion adjuvants
V. Iyer (2015)
10.1111/j.2042-7158.1982.tb04762.x
Vehicle effects on ophthalmic bioavailability: the influence of different polymers on the activity of pilocarpine in rabbit and man
M. Saettone (1982)
Discoidal niosome based controlled ocular delivery of timolol maleate.
S. Vyas (1998)
10.1208/s12249-008-9105-1
Niosome-Encapsulated Gentamicin for Ophthalmic Controlled Delivery
G. Abdelbary (2008)
10.1016/S0378-5173(02)00234-X
In vitro and in vivo evaluation of Pluronic F127-based ocular delivery system for timolol maleate.
A. El-Kamel (2002)
10.1016/J.CLAE.2013.08.133
The role of surfactants in multipurpose solutions
Valerie Franklin (2013)
10.1080/13102818.2014.997541
Effect of hydrophilic polymers on the wettability, static and dynamic, of solid substrate covered by confluent monolayer of air-damaged SIRC cells
Petar Eftimov (2015)
10.1016/j.ijpharm.2018.02.019
Mucoadhesive self-emulsifying delivery systems for ocular administration of econazole.
Ibrahim A. Elbahwy (2018)
10.1016/j.ijpharm.2016.02.027
In situ gelling systems based on Pluronic F127/Pluronic F68 formulations for ocular drug delivery.
Kosai Al Khateb (2016)
10.1016/S1350-9462(01)00017-9
Microemulsions as ocular drug delivery systems: recent developments and future challenges
T. Vandamme (2002)
10.1021/acs.molpharmaceut.7b00939
Poloxamer 407/TPGS Mixed Micelles as Promising Carriers for Cyclosporine Ocular Delivery.
M. A. Grimaudo (2018)
10.1016/J.APSB.2011.09.002
Nonionic surfactant vesicular systems for effective drug delivery—an overview
G. P. Kumar (2011)
10.3109/03639041003801885
Development of dorzolamide hydrochloride in situ gel nanoemulsion for ocular delivery
H. Ammar (2010)
10.1016/J.EURPOLYMJ.2004.07.021
The role of surfactant in controlling particle size and stability in the miniemulsion polymerization of polymeric nanocapsules
A. V. Zyl (2004)
10.3109/03639045.2015.1082582
A novel eye drop of alpha tocopherol to prevent ocular oxidant damage: improve the stability and ocular efficacy
Jiayu Xin (2016)
10.1208/s12249-009-9268-4
Nanoemulsion as a Potential Ophthalmic Delivery System for Dorzolamide Hydrochloride
H. Ammar (2009)
10.1016/j.preteyeres.2010.03.001
Preservatives in eyedrops: The good, the bad and the ugly
C. Baudouin (2010)
10.1016/j.ejps.2017.08.028
Sustained release of intravitreal flurbiprofen from a novel drug‐in‐liposome‐in‐hydrogel formulation☆
K. Pachis (2017)
10.1016/S0378-5173(01)00809-2
Effect of sodium chloride on the gelation temperature, gel strength and bioadhesive force of poloxamer gels containing diclofenac sodium.
C. Yong (2001)
10.1016/0005-2736(95)00121-I
The cationic lipid stearylamine reduces the permeability of the cationic drugs verapamil and prochlorperazine to lipid bilayers: implications for drug delivery.
Murray S. Webb (1995)
10.1007/978-3-319-41129-3_2
Nanoparticles Types, Classification, Characterization, Fabrication Methods and Drug Delivery Applications
Saurabh Bhatia (2016)
10.22377/AJP.V2I1.157
Polymers used in ocular dosage form and drug delivery systems
V. Wagh (2008)
10.1016/J.PLIPRES.2004.09.001
Oil-in-water lipid emulsions: implications for parenteral and ocular delivering systems.
S. Tamilvanan (2004)
10.3109/02652048709021825
Application of a drug delivery system to a steroidal ophthalmic preparation with lipid microspheres.
A. Yanagawa (1987)
Reduction of quaternary ammonium-induced ocular surface toxicity by emulsions: an in vivo study in rabbits
H. Liang (2008)
10.18433/J32P40
Impact of surface tension in pharmaceutical sciences.
Anahita Fathi Azarbayjani (2009)
10.1208/s12249-015-0354-5
Nanoparticle-Based Topical Ophthalmic Gel Formulation for Sustained Release of Hydrocortisone Butyrate
X. Yang (2015)
10.2174/1389450053765914
Colloidal carriers for ophthalmic drug delivery.
R. Mainardes (2005)
Mucoadhesive dexamethasone acetate-polymyxin B sulfate cationic ocular nanoemulsion--novel combinatorial formulation concept.
Xia Li (2016)
10.1517/17425247.2013.796360
Applications of poloxamers in ophthalmic pharmaceutical formulations: an overview
H. Almeida (2013)
10.1208/s12249-017-0763-8
Ocular Cubosome Drug Delivery System for Timolol Maleate: Preparation, Characterization, Cytotoxicity, Ex Vivo, and In Vivo Evaluation
Jiayuan Huang (2017)
10.1016/J.IJPHARM.2003.09.016
Vesicular systems in ocular drug delivery: an overview.
I. P. Kaur (2004)
10.1016/J.ADDR.2006.07.026
Intraocular implants for extended drug delivery: therapeutic applications.
J. Bourges (2006)
10.1016/0278-6915(95)00099-2
Ocular and dermal irritation studies of some quaternary ammonium compounds.
Guang Hai Lin (1996)
10.1016/j.ijpharm.2010.03.064
Transdermal absorption enhancement through rat skin of gallidermin loaded in niosomes.
A. Manosroi (2010)
10.1016/j.colsurfb.2014.09.042
Physicochemical characterization of epigallocatechin gallate lipid nanoparticles (EGCG-LNs) for ocular instillation.
J. Fangueiro (2014)
10.3139/113.100280
Performance of some Surfactants as Wetting Agents
M. N. Shalaby (2005)
10.1111/j.2042-7158.1994.tb03254.x
Physicochemical Characterization and Acute Toxicity Evaluation of a Positively‐charged Submicron Emulsion Vehicle
S. Klang (1994)
10.1177/026119299202000312
Prediction of Eye Irritation Potential of Surfactants using the SIRC-NRU Cytotoxicity Test
R. Roguet (1992)
10.1016/J.IJPHARM.2006.05.004
The effects of surfactants on the dissolution profiles of poorly water-soluble acidic drugs.
Sung-hyun Park (2006)
10.1089/JOP.1986.2.353
Ocular disposition of inulin from single & multiple doses of positively charged multilamellar liposomes: evidence for alterations in tear dynamics and ocular surface characteristics.
V. Lee (1986)



This paper is referenced by
Semantic Scholar Logo Some data provided by SemanticScholar