Emulsions and microemulsions for ocular drug delivery

Journal of Drug Delivery Science and Technology

Volumn 21, Issue 1, 2011, Pages 111-121

  Peng, C C ^a   Bengani, L C ^a   Jung, H J ^a   Leclerc, J ^a   Gupta, C ^a   Chauhan, A ^a  

^a J Crayton Pruitt Family Department of Biomedical Engineering   (United States)

Author keywords

Emulsions; Microemulsions; Ophthalmic drug delivery

Indexed keywords

AZITHROMYCIN; CATIONIC SURFACTANT; CYCLOSPORIN A; DIAZEPAM; DIFLUPREDNATE; DORZOLAMIDE; EVEROLIMUS; EYE DROPS; LEVOBUNOLOL; NONIONIC SURFACTANT; OLIGONUCLEOTIDE; POLYOXYETHYLENE OLEYL ETHER; RAPAMYCIN; SORBITAN LAURATE; SORBITAN OLEATE; TIMOLOL;

CLINICAL TRIAL; CONTACT LENS; DRUG DELIVERY SYSTEM; DRUG RELEASE; DRUG TARGETING; DRUG UPTAKE; DRY EYE; EMULSION; HUMAN; MICROEMULSION; NANOEMULSION; NONHUMAN; REVIEW;

EID: 79952224748     PISSN: 17732247     EISSN: None     Source Type: Journal    
DOI: 10.1016/S1773-2247(11)50010-3     Document Type: Review

References (95)

1. Winsor P.A. - Hydrotropy, solubilisation and related emulsificatoin processes 1 to 4. - Trans. Faraday Soc., 44, 376-398, 1948.
2. Shinoda K., Lindman B. - Organized surfactant systems: microemulsions. - Langmuir, 3, 135-149, 1987. (Pubitemid 17551709)
3. Hoar T.P., Schulman J.H. - Transparent water-in-oil dispersions the oleopathic hydro-micelle. - Nature, 152, 102-103, 1943.
4. Schulman J.H., Stoeckenius W., Prince L.M. - Mechanism of formation and structure of microemulsions by electron microscopy. - J. Phys. Chem., 63, 1677-1680, 1959.
5. Danielsson I., Lindman B. - The definition of microemulsion. - Colloids Surf., 3, 391-392, 1981.
6. Saettone M.F., Giannaccini B., Monti D. - Ophthalmic emulsions and suspensions. - J. Toxicol. Cutaneous Ocul. Toxicol., 20, 183-201, 2001
7. (reprinted from Pharmaceutical Emulsions and Suspensions, pp. 303-322, 2000).
8. Kawakami K., Yoshikawa T., Moroto Y., Kanaoka E., Takahashi K., Nishihara Y., Masuda K. - Microemulsion formulation for enhanced absorption of poorly soluble drugs. I. Prescription Design. - J. Control. Release, 81, 65-74, 2002.
9. Kawakami K., Yoshikawa T., Hayashi T., Nishihara Y., Masuda K. - Microemulsion formulation for enhanced absorption of poorly soluble drugs. II. In vivo study. - J. Control. Release, 81, 75-82, 2002. (Pubitemid 34454851)
10. Attwood D., Ktistis G. - A light-scattering study on oil-in-water microemulsions. - Int. J. Pharm., 52, 165-171, 1989.
11. Attwood D., Mallon C., Taylor C.J. - Phase studies on oil-in-water phospholipid microemulsions. - Int. J. Pharm., 84, R5-R8, 1992.
12. Lawrence M.J., Rees G.D. - Microemulsion-based media as novel drug delivery systems. - Adv. Drug Deliv. Rev., 45, 89-121, 2000.
13. Kayser O., Lemke A., Hernandez-Trejo N. - The impact of nanobiotechnology on the development of new drug delivery systems. - Curr. Pharm. Biotechnol., 6, 3-5, 2005.
14. Attwood D., Currie L.R.J., Elworthy P.H. - Studies of solubilized micellar solutions. I. Phase studies and particle-size analysis of solutions formed with nonionic surfactants. - J. Colloid Interface Sci., 46, 249-254, 1974.
15. Jadhav K.R., Shaikh I.M., Ambade K.W., Kadam V.J. - Applications of microemulsion based drug delivery system. - Curr. Drug Deliv., 3, 267-273, 2006.
16. Tamilvanan S. - Oil-in-water lipid emulsions: implications for parenteral and ocular delivering systems. - Prog. Lipid Res., 43, 489-533, 2004.
17. Sahoo S.K., Diinawaz F., Krishnakumar S. - Nanotechnology in ocular drug delivery. - Drug Discov. Today, 13, 144-151, 2008.
18. Vandamme T.F. - Microemulsions as ocular drug delivery systems: recent developments and future challenges. - Prog. Retin. Eye Res., 21, 15-34, 2002.
19. Kim S.H., Lutz R.J., Wang N.S., Robinson M.R. - Transport barriers in transscleral drug delivery for retinal diseases. - Ophthalmic Res., 39, 244-254, 2007. (Pubitemid 47557244)
20. Dey S., Anand B.S., Patel J., Mitra A.K. - Transporters/receptors in the anterior chamber: pathways to explore ocular drug delivery strategies. - Expert Opin. Biol. Ther., 3, 23-44, 2003.
21. Duvvuri S., Majumdar S., Mitra A.K. - Drug delivery to the retina: challenges and opportunities. - Expert Opin. Biol. Ther., 3, 45-56, 2003.
22. Koevary S.B. - Pharmacokinetics of topical ocular drug delivery: potential uses for the treatment of diseases of the posterior segment and beyond. - Curr. Drug Metab., 4, 213-222, 2003.
23. Lang J.C. - Ocular drug delivery conventional ocular formulations. - Adv. Drug Deliv. Rev., 16, 39-43, 1995.
24. Holly F.J.- Formation and rupture of the tear film. - Exp. Eye Res., 15, 515-525, 1973.
25. Farris R.L. - Tear analysis in contact lens wearers. - Tr. Am. Ophth. Soc., LXXXIII, 501-545, 1985.
26. Ronaldo M., Zierhut M. - The ocular surface and tear film and their dysfunction in dry eye disease. - Surv. Ophthalmol., 45, 203-210, 2001.
27. Chao C.C.W., Vergnes J.P., Freeman I.L., Brown S.I. - Biosynthesis and partial characterization of tear film glycoproteins. Incorporation of radioactive precursors by human lacrimal gland explants in vitro. - Exp. Eye Res., 30, 411-425, 1980.
28. Ruiz-Ederra J., Levin M.H., Verkman A.S. - In situ fluorescence measurement of tearfilm [Na+], [K+], [CI-], and pH in mice shows marked hypertonicity in aquasporin-5 deficiency. - IOVS, 50, 2132-2138, 2009.
29. Hosoya K.I., Lee. V.H.L., Kim K.J. - Roles of the conjunctiva in ocular drug delivery: a review of conjunctival transport mechanism and their regulation. - Eur. J. Pharm. Biopharm., 60, 227-240, 2005.
30. Le Bourlais C., Acar L., Zia H., Sado P.A., Needham T., Leverge R. - Ophthalmic drug delivery systems, Recent advances. - Prog. Retin. Eye Res., 17, 33-58, 1998.
31. Joussen A.M., Rohrschneider K., Reichling J., Kirchhof B., Kruse F.E. -Treatment of corneal neovascularization with dietary isoflavonoids and flavonoids. - Exp. Eye Res., 71, 483-487, 2000.
32. Fialho S.L., da Silva-Cunha A. - New vehicle based on a microemulsion for topical ocular administration of dexamethasone. - Clin. Exp. Ophthalmol., 32, 626-632, 2004.
33. Buech G., Bertelmann E., Pleyer U., Siebenbrodt I., Borchert H.H. - Formulation of sirolimus eye drops and corneal permeation studies. - J. Ocul. Pharma. Ther., 23, 292-303, 2007.
34. Siebenbrodt I., Keipert S. - Poloxamer-systems as potential ophthalmics II: microemulsions, - Eur. J. Pharm. Biopharm., 39, 25-30, 1993.
35. Baspinar Y., Bertelmann E., Pleyer U., Buech G., Siebenbrodt I., Borchert H.H. - Corneal permeation studies of everolimus microemulsion. - J. Ocul. Pharm. Ther., 24, 399-402, 2008.
36. Kirchner G.I., Meier-Wiedenbach I., Manns M.P. - Clinical pharmacokinetics of everolimus. - Clin. Pharmacokinet., 43, 83-95, 2004.
37. Kovarik J.M., Tedesco H., Pascual J., Civati G., Bizot M.N., Geissler J., Schmidli H. - Everolimus therapeutic concentration range defined from a prospective trial with reduced-exposure cyclosporine in de novo kidney transplantation. - Ther. Drug Monit., 26, 499-505, 2004.
38. Starling R.C., Hare J.M., Hauptman P., McCurry K.R., Mayer H.W., Kovarik J.M., Schmidli H. - Therapeutic drug monitoring for everolimus in heart transplant recipients based on exposure-effect modeling. - Am. J. Transplant., 4, 2126-2131, 2004.
39. Klang S., Abdulrazik M., Benita S. - Influence of emulsion droplet surface charge on indomethacin ocular tissue distribution. - Pharm. Dev. Technol., 5, 521-532, 2000.
40. Liu Y., Lin X., Tang X. - Lipid emulsions as a potential delivery system for ocular use of azithromycin. - Drug Dev. Ind. Pharm., 35, 887-896, 2009.
41. Attwood D., Mallon C., Ktistis G., Taylor C.J. - A study on factors influencing the droplet size in nonionic oil-in-water microemulsions. - Int. J. Pharm., 88, 417-422, 1992.
42. Liang H., Brignole-Baudouin F., Rabinovich-Guilatt L., Mao Z., Riancho L., Faure M.O., Warnet J.M., Lambert G., Baudouin C. - Reduction of quaternary ammonium-induced ocular surface toxicity by emulsions: an in vivo study in rabbits. - Mol. Vis., 14, 204-216, 2008.
43. Liang H., Baudouin C., Faure M.O., Lambert G., Brignole-Baudouin F. - Comparison of the ocular tolerability of a latanoprost cationic emulsion versus conventional formulations of prostaglandins: an in vivo toxicity assay. - Mol. Vis., 15, 1690-1699, 2009.
44. Sznitowska M., Zurowska-Pryczkowska K., Dabrowska E., Janicki S. - Increased partitioning of pilocarpine to the oily phase of submicron emulsion does not result in improved ocular bioavailability. - Int. J. Pharm., 202, 161-164, 2000.
45. Yamaguchi M., Ueda K., Isowaki A., Ohtori A., Takeuchi H., Ohguro N., Tojo K. - Mucoadhesive properties of Chitosan-coated ophthalmic lipid emulsion containing indomethacin in tear fluid. - Biol. Pharm. Bull., 32, 1266-1271, 2009.
46. Goto E., Shimazaki J., Monden Y., Takano Y., Yagi Y., Shimmura S., Tsubota K. - Low-concentration homogenized castor oil eye drops for noninflamed obstructive meibomian gland dysfunction. - Ophthalmology, 109, 2030-2035, 2002. (Pubitemid 35222556)
47. Ammar H.O., Salama H.A., Ghorab M., Mahmoud A.A. - Nanoemulsion as a potential ophthalmic delivery system for dorzolamide hydrochloride. - AAPS Pharmscitech., 10, 808-819, 2009.
48. Carlfors J., Edsman K., Petersson R., Jornving K. - Rheological evaluation of Gelrite in situ gels for ophthalmic use. - Eur. J. Pharm. Sci., 6, 113-119, 1998.
49. Sanzgiri Y.D., Maschi S., Crescenzi V., Callegaro L., Topp E.M., Stella V.J. - Gellan-based systems for ophthalmic sustained delivery of methylprednisolone. - J. Control. Release, 26, 195-201, 1993.
50. Rozier A., Mazuel C., Grove J., Plazonnet B. - Functionality testing of Gellan gum, a polymeric excipient material for ophthalmic dosage forms. - Inter. J. Pharm., 153, 191-198, 1997.
51. Gan L., Gan Y., Zhu C.L., Zhang X.X., Zhu J.B. - Novel microemulsion in situ electrolyte-triggered gelling system for ophthalmic delivery of lipophilic cyclosporine A: in vitro and in vivo results. - Int. J. Pharm., 365, 143-149, 2009.
52. Alany R.G., Tucker I.G., Davies N.M., Rades T. - Characterizing colloidal structures of pseudoternary phase diagrams formed by oil/water/amphiphile systems. - Drug Dev. Ind. Pharm., 27, 31-38, 2001.
53. Chan J., Maghraby G.M.E., Craig J.P., Alany R.G. - Effect of water-in-oil microemulsions and lamellar liquid crystalline systems on the precorneal tear film of Albino New Zealand rabbits. - Clin. Ophthalmol., 2, 129-137, 2008.
54. Chan J., El Maghraby G.M.M., Craig J.P., Alany R.G. - Phase transition water-in-oil microemulsions as ocular drug delivery systems: in vitro and in vivo evaluation. - Int. J. Pharm., 328, 65-71, 2007.
55. Alany R.G., Rades T., Nicoll J., Tucker I.G., Davies N.M. - W/O microemulsions for ocular delivery: evaluation of ocular irritation and precorneal retention. - J.Control. Release, 111, 145-152, 2006.
56. Zhu H., Chauhan A. - A mathematical model for ocular tear and solute balance. - Curr. Eye Res., 30, 841-854, 2005.
57. Zhu H., Chauhan A. - A mathematical model for tear drainage through the canaliculi. - Curr. Eye Res., 30, 621-630, 2005.
58. Gupta C., Chauhan A. - Drug transport in HEMA contunctival inserts containing precipitated drug particles. - J.Colloid Interface Sci., 347, 31-42, 2010.
59. Ibrahim S.S., Awad G.A.S., Geneidi A., Mortada N.D. - Comparative effects of different cosurfactants on sterile prednisolone acetate ocular submicron emulsions stability and release. - Colloids Surf., B, 69, 225-231, 2009.
60. Benita S., Levy M.Y. - Submicron emulsions as colloidal drug carriers for intravenous administration, Comprehensive physicochemical characterization. - J. Pharm. Sci., 82, 1069-1079, 1993.
61. Langevin D., Meunier J., Cazabat A.M. - Microemulsions. - Recherche, 16, 720-728, 1985.
62. Abelson M.B., Udell I.J., Weston J.H. - Normal human tear pH by direct measurement. - Arch. Ophthalmol., 99, 301-301, 1981.
63. Carney L.G., Hill R.M. - Human tear pH: diurnal variations. - Arch. Ophthalmol., 94, 821-824, 1976.
64. Fischer F.H., Wiederholt M. - Human pre-corneal tear film pH measured by microelectrodes. - Graefe's Arch. Clin. Exp. Ophthalmol., 218, 168-170, 1982.
65. Sznitowska M., Zurowska-Pryczkowska K., Janicki S., Jarvinen T. - Miotic effect and irritation potential of pilocarpine prodrug incorporated into a submicron emulsion vehicle. - Int. J. Pharm., 184, 115-120, 1999.
66. Gallarate M., Gasco M.R., Trotta M., Chetoni P., Saettone M.F. - Preparation and evaluation in-vitro of solutions and o/w microemulsions containing levobunolol as ion-pair. - Int. J. Pharm., 100, 219-225, 1993.
67. Felt O., Furrer P., Mayer J.M., Plazonnet B., Buri P., Gurny R. - Topical use of chitosan in ophthalmology: tolerance assessment and evaluation of precorneal retention. - Int. J. Pharm., 180, 185-193, 1999.
68. Calvo P., Remunan-Lopez C., Vila-Jato J.L., Alonso M.j. - Development of positively charged colloidal drug carriers: chitosan-coated polyester nanocapsules and submicron-emulsions. - Colloid. Polym. Sci., 275, 46-53, 1997.
69. Radomska-Soukharev A., Wojciechowska J. - Microemulsions as potential ocular drug delivery systems: phase diagrams and physical properties depending on ingredients. - Acta Pol. Pharm., 62, 465-471, 2005.
70. Lv F.F., Zheng L.Q., Tung C.H. - Phase behavior of the microemulsions and the stability of the chloramphenicol in the microemulsion-based ocular drug delivery system. - Int. J. Pharm., 301, 237-246, 2005.
71. Sasaki H., Yamamura K., Nishida K., Nakamura J., Ichikawa M. - Delivery of drugs to the eye by topical application. - Prog. Retin. Eye Res., 15, 583-620, 1996.
72. Rabinovich-Guilatt L., Couvreur P., Lamber G., Goldstein D., Benita S., Dubernet C. - Extensive surface studies help to analyse zeta potential data: the case of cationic emulsions. - Chem. Phys. Lipids, 31, 1-13, 2004.
73. Hagigit T., Nassar T., Behar-Cohen F., Lambert G., Benita S. - The influence of cationic lipid type on in vitro release kinetics profiles of antisense oligonucleotide from cationic nanoemulsions. - Eur. J. Pharm. Biopharm., 70, 248-259, 2008.
74. Hagigit T., Abdulrazik M., Orucov F., Valamanesh F., Lambert M., Lambert G., Behar-Coehn F., Benita S. - Topical and intravitreous administration of cationic nanoemulsions to deliver antisense oligonucleotides directed towards VEGF KDR receptors to the eye. - J. Control. Release, 145, 297-305, 2010.
75. Creech J.L., Chauhan A., Radke C.J. - Dispersive mixing in the posterior tear film under a soft contact lens. - Ind. Eng. Chem. Res., 40, 3015-3026, 2001.
76. McNamara N.A., Poise K.A., Brand R.J., Graham A.D., Chan J.S., McKenney C.D. - Tear mixing under a soft contact lens: Effects of lens diameter. - Am. J. Ophthalmol., 127, 659-665, 1999.
77. Karlgard C.C.S., Wong N.S., Jones L.W., Moresoli C. - In vitro uptake and release studies of ocular pharmaceutical agents by silicon-containing and p-HEMA hydrogel contact lens materials. - Int. J. Pharm., 257, 141-151, 2003.
78. Gulsen D., Chauhan A. - Dispersion of microemulsion drops in HEMA hydrogel: a potential ophthalmic drug delivery vehicle. - Int. J. Pharm., 292, 95-117, 2005.
79. Gulsen D., Chauhan A. - Ophthalmic drug delivery through contact lenses. - Invest. Ophthalmol. Vis. Sci., 45, 2342-2347, 2004.
80. Li C.C., Abrahamson M., Kapoor Y., Chauhan A. - Timolol transport from microemulsions trapped in HEMA gels. - J. Colloid Interface Sci., 315, 297-306, 2007.
81. Kapoor Y., Chauhan A. - Ophthalmic delivery of cyclosporine A from Brij-97 microemulsion and surfactant-laden p-HEMA hydrogels. - Int. J. Pharm., 361, 222-229, 2008.
82. http://www.fda.gov/Drugs/InformationOnDrugs/ucm129662.htm, - Approved drug products with therapeutic equivalence evaluations (orange book), US Food and Drug Administration.
83. www.restasis.com
84. Lallemand F., Felt-Baeyens O., Besseghir K., Behar-Cohen F., Gurny R. - Cyclosporine A delivery to the eye: a pharmaceutical challenge. - Eur. J. Pharm. Biopharm., 56, 307-318, 2003.
85. Stevenson D., Tauber J., Reis B.L. et al. - Efficacy and safety of cyclosporin A ophthalmic emulsion in the treatment of moderate-to-severe dry eye disease, A dose-ranging, randomized trial. - Ophthalmology, 107, 967-974, 2000.
86. Sall K., Stevenson O.D., Mundorf T.K., Reis B.L. et al. - Two multicenter, randomized studies of the efficacy and safety of cyclosporine ophthalmic emulsion in moderate to severe dry eye disease. - Ophthalmology, 107, 631-639, 2000. (Pubitemid 30191329)
87. Hom M.M. - Use of cyclosporine 0.05% ophthalmic emulsion for contact lens-intolerant patients. - Eye Contact Lens, 32, 109-111, 2006. (Pubitemid 44510058)
88. Willen C.M., McGwin G., Liu B., Owsley C., Rosenstiel C. - Efficacy of cyclosporine 0.05% ophthalmic emulsion in contact lens wearers with dry eyes. - Eye Contact Lens, 34, 43-45, 2008.
89. http://www.fda.gov/downloads/Drugs/ GuidanceComplianceRegulatoryInformation/EnforcementActivitiesbyFDA/ WarningLettersandNoticeofViolationLetterstoPharmaceutical-Companies/UCM204946. pdf.
90. www.alcon.com
91. Kimura M., Yasueda S., Yamaguchi M., Inada K. - compositions containing difluprednate. - US Patent 6,114,319.
92. Scaffidi R.C., Korb D.R. - Comparison of the efficacy of two lipid emulsion eyedrops in increasing tear film lipid layer thickness. - Eye Contact Lens, 33, 38-44, 2007. (Pubitemid 46114827)
93. http://www.refreshbrand.com/
94. http://www.alimerasciences.com/Portals/0/News-releases-080107.pdf.
95. Korb D.R., Scaffidi R.C., Greiner J.V., Kenyon K.R., Herman J.P., Blackie C.A., Glonek T., Case C.L., Finnemore V.M., Douglass T. - The effect of two novel lubricant eye drops on tear film lipid layer thickness in subjects with dry eye symptoms. - Optom. Vis. Sci., 82, 594-601, 2005.