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Brimonidine Formulation In Polyacrylic Acid Nanoparticles For Ophthalmic Delivery

T. K. De, D. Rodman, B. Holm, P. Prasad, E. Bergey
Published 2003 · Materials Science

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In ocular drug delivery, a major problem is providing an adequate concentration of a therapeutic agent in the precorneal area. Mucoadhesive carriers such as polyacrylic acid in sub-colloidal, nanoparticulate form, have a strong potential for ophthalmic drug delivery. A formulation of brimonidine loaded in polyacrylic acid nanoparticles has been prepared for potential delivery in ophthalmic therapy. The particles were prepared by a reverse microemulsion polymerization technique and their sizes were in the range of 50 nm. In a preliminary biocompatibility test, Caco-2 cells (human primary colonic tumour adenocarcinoma) and human corneal epithelial cells incubated with polyacrylic acid nanoparticles were found to retain their viability over varying times. The loading efficiency of the drug brimonidine in the particles was shown to be between 80–85% and pH dependent. The bioadhesive polyacrylic hydrogel nanoparticles, used in the present study, exhibited superior loading properties for brimonidine, and the formulation was stable for more than 5 weeks. When the drug-loaded nanoparticles were dispersed in a phosphate buffer saline (pH = 7.4), the drug was slowly released over several hours. Two-photon laser scanning microscopic studies of dye-conjugated polyacrylic acid nanoparticles demonstrated the accumulation of the particles on the surface and intercellular spaces of Caco-2 cells.
This paper references
10.1016/0378-5173(96)04624-8
Study of β-cyclodextrin and ethylated β-cyclodextrin salbutamol complexes, in vitro evaluation of sustained-release behaviour of salbutamol
V. Lemesle-Lamache (1996)
10.1016/S0039-6257(96)82027-3
Preclinical evaluation of brimonidine.
J. Burke (1996)
Binding of acrylic polymers to mucin/epithelial surfaces: structure-property relationships.
J. M. Gu (1988)
Ion eschange resins
XI S.HA (1994)
10.1023/A:1016213405081
Mucoadhesive Polymers in Peroral Peptide Drug Delivery. II. Carbomer and Polycarbophil Are Potent Inhibitors of the Intestinal Proteolytic Enzyme Trypsin
H. L. Luessen (2004)
10.1016/S0002-9394(98)00286-4
Brimonidine tartrate 0.2% twice daily vs timolol 0.5% twice daily: 1-year results in glaucoma patients. Brimonidine Study Group.
L. Katz (1999)
10.1016/S0168-3659(96)01626-4
Mechanisms of buccal mucoadhesion of novel copolymers of acrylic acid and polyethylene glycol monomethylether monomethacrylate
A. H. Shojaei (1997)
Almc>\cri.i., 13. and Ciiiis, I
S J. (1997)
10.1016/S0161-6420(97)30349-2
Brimonidine tartrate: a one-month dose response study.
R. Derick (1997)
A comparison of the safety and efficacy of brimonidine 0.2'%,. BID versus 'I'ID in subjects with elevated intraocular pressure
L A. (1996)
10.1002/JPS.2600680606
Mechanistic and quantitative evaluation of precorneal pilocarpine disposition in albino rabbits.
V. Lee (1979)
10.1106/17CP-23JM-Y3R4-GUYG
An Ophthalmic Formulation of a Beta-Adrenoceptor Antagonist, Levobetaxolol, Using Poly(Acrylic Acid) Nanoparticles as Carrier: Loading and Release Studies
T. K. De (2001)
10.1002/jps.2600650909
Quantitative precorneal disposition of topically applied pilocarpine nitrate in rabbit eyes.
T. Patton (1976)
10.1016/S0168-3659(96)01536-2
Mucoadhesive polymers in peroral peptide drug delivery. IV. Polycarbophil and chitosan are potent enhancers of peptide transport across intestinal mucosae in vitro
H. L. Luessen (1997)
10.1111/j.2042-7158.1991.tb03534.x
Improvement of Ocular Penetration of Amikacin Sulphate by Association to Poly(butylcyanoacrylate) Nanoparticles
C. Losa (1991)
T h e efficacy of brimonidine in preventing intraocular pressure elevation in the provocative test for primary angle-closure glaucoma
C K. (2002)
10.3109/03639049709148498
Mucoadhesive Drug Delivery Systems
A. Ahuja (1997)
10.1016/0378-5173(78)90037-6
An ‘in vitro’ system for the correlation of drug/protein binding with variable plasma protein profile
D. Harron (1978)
Mechanism of mucoadhcsion of poly(:icrylic acid) hydrogels. Plrarmciceictical Hesearclr, 4, 457-464. applied pilocarpine nitrate in rabbit eyes
H IaposA (1987)
10.1016/S0161-6420(98)91048-X
Twelve-month results of an ongoing randomized trial comparing brimonidine tartrate 0.2% and timolol 0.5% given twice daily in patients with glaucoma or ocular hypertension. Brimonidine Study Group 2.
R. Leblanc (1998)
Mucoadhe peptide drug delivery. ct of poly(acrylates) on enzymatic dcgradation o f peptide drugs by intestinal brush border membrane vesicles
I H k I (1995)
10.1111/j.2042-7158.1997.tb06103.x
Bioadhesive Microspheres for Ophthalmic Administration of Acyclovir
I. Genta (1997)
10.1089/JOP.1994.10.57
Ion exchange resins for ophthalmic delivery.
R. Jani (1994)
ILanier and I,. Limbird (Reading, U I C Hal-wood Academic Publishers)
Correlation between oral absorption in humans and apparent drug permeability coefficients in human intestinal epithelial (Caco-2) cell culture
P Aiviwiltsson (1991)
Mechanistic and quantitative evaluation
H. Id (1979)
Ongoing clinical assessment of the safety protile and efficacy of brimonidine compared with timolol: year-three results
M SMIXMI (2000)
10.1001/ARCHOPHT.1995.01100010079024
The cardiovascular, pulmonary, and ocular hypotensive effects of 0.2% brimonidine.
J. Nordlund (1995)
10.1016/S0378-5173(97)04904-1
Textural, viscoelastic and mucoadhesive properties of pharmaceutical gels composed of cellulose polymers
D. Jones (1997)
10.1016/0142-9612(95)00307-X
Hydrogels as mucoadhesive and bioadhesive materials: a review.
N. Peppas (1996)
10.1016/0928-0987(95)00042-9
MUCOADHESIVE POLYMERS IN PERORAL PEPTIDE DRUG DELIVERY. I. INFLUENCE OF MUCOADHESIVE EXCIPIENTS ON THE PROTEOLYTIC ACTIVITY OF INTESTINAL ENZYMES
H. L. Luessen (1996)
10.1006/EXER.2001.1122
Neuroprotective effects of brimonidine against transient ischemia-induced retinal ganglion cell death: a dose response in vivo study.
M. P. Lafuente (2002)
Quantitative precorncal disposition of topical
J R. (1976)
10.1016/S0149-2918(00)87981-3
Ongoing clinical assessment of the safety profile and efficacy of brimonidine compared with timolol: year-three results. Brimonidine Study Group II.
S. Melamed (2000)
10.1081/BIO-100001254
A REVERSE MICROEMULSION POLYMERIZATION METHOD FOR PREPARATION OF BIOADHESIVE POLYACRYLIC ACID NANOPARTICLES FOR MUCOSAL DRUG DELIVERY: LOADING AND RELEASE OF TIMOLOL MALEATE
T. de (2001)
Improvement of ocular penetration of aniikacin sulphate by association to poly(biitylcyanoacryl~itc) nanoparticlcs. Tlie Joirrrrnl of Pharrnacji arid
I CNiLEI (1991)
10.1016/0378-5173(92)90043-2
Bioadhesion: The effect of polyacrylic acid on the ocular bioavailability of timolol
F. Thermes (1992)
10.1111/J.1600-0420.1996.TB00086.X
Viscous carbomer eye drops in patients with dry eyes. Efficacy and safety. A randomized, open, cross-over, multicentre study.
K. Marner (1996)
10.1021/JS950474+
Comparative in vitro evaluation of several colloidal systems, nanoparticles, nanocapsules, and nanoemulsions, as ocular drug carriers.
P. Calvo (1996)
10.1016/0378-5173(96)04665-0
In-vitro bioadhesion of carbopol hydrogels
H. Blanco-Fuente (1996)
10.1023/A:1018995923348
Pharmacokinetic and Pharmacodynamic Aspects of an Ophthalmic Pilocarpine Nanoparticle-Delivery-System
A. Zimmer (2004)
Analogs of U K 14,304: structural features responsible for ct2-adrenoceptor activity
M SAMU (1995)
10.1016/S0016-5085(89)80072-1
Characterization of the human colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability.
I. Hidalgo (1989)
Cell cultures as models for drug absorption across the intestinal mucosa.
P. Artursson (1991)
10.1016/0378-5173(96)04613-3
Mucoadhesive polymers in peroral peptide drug delivery. V. Effect of poly(acrylates) on the enzymatic degradation of peptide drugs by intestinal brush border membrane vesicles
Henrik L. Lueβen (1996)
10.1016/S0169-409X(00)00120-4
Mucoadhesive nanoparticulate systems for peptide drug delivery.
H. Takeuchi (2001)
Testural, viscoelastic and mucoadhesive properties of pharmaceutical gels composed of cellulosc polymers
A F. (1997)
10.1016/0006-291X(91)91647-U
Correlation between oral drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelial (Caco-2) cells.
P. Artursson (1991)
10.1023/A:1015856223252
Mucoadhesion of Copolymers and Mixtures Containing Polyacrylic Acid
F. Thermes (2004)
10.1016/S0378-5173(97)00297-4
Evaluation of possible mechanism(s) of bioadhesion
Khalid Mahrag Tur (1998)
Viscous carbomer eyes: e f i c a c y and safety: a randomized, open, crossover, multicentre study. Act0 Ophthmlrrrologica Sccitrdiriavica
R4 Iiasi-Pisi (1996)
Receptors: Structure, Function and Therapeutic Implications, edited b y S. ILanier and I
J M. (1996)
Brimonidine tartrate: a onemonth dose response study
J F. (1997)
Cell cultures as models for drug absorption across the intestinal m u c~s a . Critical Reviezos in Therapeutic Drug Carrier Systems
P Ailttursson (1991)
[Treatment of dry eye syndrome with lacrimal gel: a randomized multicenter study].
L. Laroche (1991)
10.1523/JNEUROSCI.08-07-02618.1988
Basic and acidic fibroblast growth factors have trophic effects on neurons from multiple CNS regions
P. Walicke (1988)
A comparison of the safety and efficacy of twice daily brimonidine 0.2% versus bctasolol 0.25'%) in subjects with elevatcd intraocular pressure. T h e Brimonidinc Studp Group I l l
J Siiiic (1996)
and chitosan are potent enhancers of peptide transport across intestinal mucosiie in vitro
H I LiIcuv (1997)
10.1097/00003226-199807000-00015
Carbomer- versus cellulose-based artificial-tear formulations: morphologic and toxicologic effects on a corneal cell line.
Y. Diebold (1998)
10.1016/0378-5173(86)90037-2
Optimization of pilocarpine loading onto nanoparticles by sorption procedures
T. Harmia (1986)
10.1517/13543784.6.8.1063
Pulmonary-Allergy, Dermatological, Gastrointestinal and Arthritis. Brimonidine
L. Cantor (1997)
Poly(acrylic acid) microparticles widen the intercellular spaces of Caco-2 cell monolayers : An examination by confocal laser scanning microscopy
B. Kriwet (1996)
10.1016/S0002-9394(99)00076-8
Acute versus chronic effects of brimonidine on aqueous humor dynamics in ocular hypertensive patients.
C. Toris (1999)
10.1016/S0039-6257(96)82030-3
A Comparison of the Safety and Efficacy of Twice Daily Brimonidine 0.2% Versus Betaxolol 0.25% in Subjects with Elevated Intraocular Pressure
J. Serle (1996)
10.1007/BF01204617
Lubrithal® (Leo viscous eye gel), precorneal residence time in normal and dry eyes
S. Al-Mansouri (2005)
Brimonidine tartrate
L J. (1999)
10.1016/0960-894X(95)00295-5
Analogs of UK 14,304: Structural features responsible for α2 adrenoceptor activity
S. A. Munk (1995)
10.1089/108076802317373851
The efficacy of brimonidine in preventing intraocular pressure elevation in the provocative test for primary angle-closure glaucoma.
Yuh-Fang Chen (2002)
10.1111/j.2042-7158.1996.tb03911.x
Improved Ocular Bioavailability of Indomethacin by Novel Ocular Drug Carriers
P. Calvo (1996)
10.1023/A:1016467219657
Mechanisms of Mucoadhesion of Poly(acrylic Acid) Hydrogels
H. Park (2004)
Improved ocular penetration of gentamicin by mucoadhesive polymer polycarbophil in the pigmented rabbit.
C. Lehr (1994)
I n vitro bioadhcsion of carbopol hydrogels
U I A Ni . C Ia (1996)
Basic and acidic fibroblast growth factors have tropic effect on neurons from multiple C
P A (1988)
10.1016/S0378-5173(97)00256-1
Methylmethacrylate sulfopropylmethacrylate copolymer nanoparticles for drug delivery: Part II: arecaidine propargyl ester and pilocarpine loading and in vitro release
K. Langer (1997)
10.1016/S0039-6257(96)82029-7
Clinical experience with brimonidine 0.2% and timolol 0.5% in glaucoma and ocular hypertension.
J. Schuman (1996)
h'tucoadliesive drug delivery systems
K KharR. (1997)
10.1016/0378-5173(83)90157-6
Structural requirements of muscarine, 1,3-dioxolane and their analogues for agonist activity at cholinergic receptors
R. Timoney (1983)
10.1001/ARCHOPHT.1997.01100160017002
A 1-year study of brimonidine twice daily in glaucoma and ocular hypertension. A controlled, randomized, multicenter clinical trial. Chronic Brimonidine Study Group.
J. Schuman (1997)



This paper is referenced by
10.1201/9781420008449.CH13
Pharmaceutical Applications of Nanoparticulate Drug-Delivery Systems
Y. Pathak (2007)
10.1016/J.EJPB.2007.08.001
Nanoparticles for drug delivery: the need for precision in reporting particle size parameters.
M. Gaumet (2008)
10.3109/9781420078053
Drug Delivery Nanoparticles Formulation and Characterization
Y. Pathak (2009)
10.1016/J.ACA.2004.01.059
Miniaturized reference electrodes with stainless steel internal reference elements
Jeremy P. Wilburn (2004)
10.1002/APP.39788
In situ gelling ophthalmic drug delivery system: Formulation and evaluation
Neeraj Mittal (2014)
10.1504/IJNP.2011.043501
Nanoparticles: a boon for modernisation of drug delivery: a review
Mohammed Shuaib Khan (2011)
10.1016/B978-012370585-3.50004-2
Drug Delivery Systems in Ophthalmic Applications
A. L. Weiner (2008)
10.1080/02652040400008515
Polycarboxylic acid nanoparticles for ophthalmic drug delivery: an ex vivo evaluation with human cornea
T. K. De (2004)
10.1007/978-1-59745-375-2_22
Ophthalmic Applications of Nanotechnology
Swita Raghava (2008)
10.1017/S1431927619000448
Effect of Ultra-Small Chitosan Nanoparticles Doped with Brimonidine on the Ultra-Structure of the Trabecular Meshwork of Glaucoma Patients.
Indu Barwal (2019)
10.1109/WARTIA.2014.6976197
Strength property and structural analysis of material from fibers and acrylic emulsion terpolymer
H. Wu (2014)
10.1007/s11095-006-9087-1
Development of a Novel Method for the Preparation of Thiolated Polyacrylic Acid Nanoparticles
M. Greindl (2006)
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