Abstract
Association of Carbopol 934P and Carbopol 1342 (a hydrophobic modified Carbopol resin) with phospholipid vesicles was assessed by photon correlation spectroscopy and microelectrophoresis at pH 7.4 and 5. The precorneal clearance of the polymer-coated vesicles was compared to that of uncoated vesicles by lacrimal dacryoscintigraphy in the rabbit. The mucoadhesive polymer-coated vesicles demonstrated significantly enhanced precorneal retention compared to noncoated vesicles only at pH 5 (P < 0.005). The entrapment and subsequent release of tropicamide from Carbopol 1342-coated and uncoated liposomes were determined in vitro together with an in vivo evaluation of the vesicles formulated at the lower pH. Mucoadhesive polymer-coated vesicles failed to increase significantly the bioavailability of the entrapped tropicamide compared to uncoated vesicles and aqueous solution.
Similar content being viewed by others
REFERENCES
N. M. Davies, S. J. Farr, J. Hadgraft, and I. W. Kellaway. Evaluation of mucoadhesive polymers in ocular drug delivery. I. Viscous solutions. J. Pharm. Res. 8:1039–1043 (1991).
G. Smolin, M. Okumoto, S. Feilere, and D. Condon. Idoxuridine-liposome therapy for herpes simplex keratites. Am. J. Ophthalmol. 91:220–225 (1981).
H. E. Schaeffer and D. C. Krohn. Liposomes in topical drug delivery. Invest. Ophthalmol. Vis. Sci. 21:220–227 (1982).
K. Singh and M. Mezei. Liposomal ophthalmic drug delivery. I. Triamcinolone acetonide. Int. J. Pharm. 16:339–344 (1983).
K. Singh and M. Mezei. Liposomal ophthalmic drug delivery. II. Dihydrostreptomycin sulfate. Int. J. Pharm. 19:263–269 (1984).
R. E. Stratford, D. C. Young, M. A. Ridell, and V. H. L. Lee. Ocular distribution of liposome encapsulated epinephrine and inulin in the albino rabbit. Curr. Eye Res. 2(6):377–386 (1982/3).
S. Benita, J. D. Plenecassagne, G. Cavé, D. Drouin, P. Le Hao Dong, and D. Sincholle. Pilocarpine hydrochloride liposomes: Characterization in vitro and preliminary evaluation in vivo in rabbit eye. J. Microencapsul. l(3):203–216 (1984).
D. Meisner, J. Pringle, and M. Mezei. Liposomal ophthalmic drug delivery. III. Pharmacodynamic and biodisposition studies of atropine. Int. J. Pharm. 55:105–113 (1989).
P. Fitzgerald. Ph.D. thesis, University of Nottingham, Nottingham, UK, 1985.
G. P. Martin, I. W. Kellaway, and C. Marriott. The solubilization of progesterone by mixed bile salt-phospholipid solutions. Chem. Phys. Lipids 22:227–238 (1978).
S. J. Farr, I. W. Kellaway, D. R. Parry-Jones, and S. G. Woolfrey. 99m-Technetium as a marker of liposomal deposition and clearance in the human lung. Int. J. Pharm. 26:303–316 (1985).
W. G. Love, N. Amos, B. D. Williams, and I. W. Kellaway. High performance liquid chromatographic analysis of liposome stability. J. Microencapsul. 7:105–112 (1990).
R. Y. Lockhead, W. J. Heniker, and J. Y. Castaneda. Hydro-phobically modified Carbopol resins. Soap Cosmet. Chem. Spec. 63:28–33 (1987).
K. Seki and D. A. Tirrell. pH-dependent complexation of poly-derivatives with phospholipid vesicle membranes. Macromolecules 17:1692–1698 (1984).
H. S. Ch'ng, H. Park, P. Kelly, and J. R. Robinson. Bioadhesive polymers as platforms for oral controlled drug delivery. II. Synthesis and evaluation of some swelling water-insoluble bioadhesive polymers. J. Pharm. Sci. 74:399–405 (1985).
H. Park and J. R. Robinson. Physico-chemical properties of water insoluble polymers important to mucin/epithelial adhesion. J. Control. Release 2:47–57 (1985).
L. J. Kerr, I. W. Kellaway, J. D. Lewis, D. R. Kelly, and G. D. Parr. The interaction of polyacrylic acid with gastric glycoprotein. Proc. Int. Symp. Control. Rel. Bioact. Mater. 16:400–401 (1989).
L. J. Kerr, I. W. Kellaway, and G. D. Parr. The interaction of bioadhesive polymers with gastric glycoproteins. J. Pharm. Pharmacol. 41:143P (1989).
S. E. G. Nilsson and S. Latkovic. A difference in phagocytic capability between the corneal and conjunctival epithelium in the cornea in health and disease. In P. D. Trevor-Roper (ed.), VIth Congress of the European Society of Ophthalmology, Academic Press, London, 1981, p. 21.
V. H. L. Lee, K. A. Takemoto, and D. S. Iimoto. Precorneal factors influencing the ocular distribution of topically applied liposomal inulin. Curr. Eye Res. 3:585–591 (1984).
P. Fitzgerald, J. Hadgraft, J. Kreuter, and C. G. Wilson. A gamma-scintigraphic evaluation of microparticulate ophthalmic delivery systems: Liposomes and nanoparticles. Int. J. Pharm. 40:81–84 (1987).
P. Fitzgerald, J. Hadgraft, and C. G. Wilson. A gamma-scintigraphic evaluation of the precorneal residence of liposomal formulations in the rabbit. J. Pharm. Pharmacol. 39:487–490 (1987).
K. Taniguchi, N. Yamazama, K. Itakura, K. Morisaki, and S. Hayashi. Partition characteristics and retention of anti-inflammatory steroids in liposomal ophthalmic preparations. Chem. Pharm. Bull. 35(3): 1214–1222 (1987).
F. Defrise-Quertain, P. Chatelain, J. M. Raysschaert, and M. Delmelle. Spin label partitioning in lipid vesicles: A model study for drug encapsulation. Biochim. Biophys. Acta. 628:57–68 (1980).
R. D. Schoenwald and V. F. Smolen. Drug absorption analysis from pharmacological data. III. Transcorneal, biophasic availability of tropicamide. J. Pharm. Sci. 60:1029–1045 (1971).
R. F. Barber and P. N. Shek. Liposomes and tear fluid. I. Release of vesicle-entrapped carboxyfluorescein. Biochim. Biophys. Acta 879:157–163 (1986).
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Davies, N.M., Farr, S.J., Hadgraft, J. et al. Evaluation of Mucoadhesive Polymers in Ocular Drug Delivery. II. Polymer-Coated Vesicles. Pharm Res 9, 1137–1144 (1992). https://doi.org/10.1023/A:1015891419676
Issue Date:
DOI: https://doi.org/10.1023/A:1015891419676