Skip to main content
SpringerLink
Log in

Poly(ε-Caprolactone) Nanocapsules in Carteolol Ophthalmic Delivery

  • Published:
Pharmaceutical Research Aims and scope Submit manuscript

Abstract

In order to increase the ocular absorption of carteolol, this antiglaucomatous drug was incorporated into either nanoparticles (NP) or nanocapsules (NC). The polymer used was poly(ε-caprolactone) (PCL). The dosage forms were tested on intraocular hypertensive-induced rabbits. Results are presented as the chronological variations of the intraocular pressure (IOP) in comparison with the commercial aqueous solution (Carteol eye drops). The therapeutic results (decrease in IOP) were much more pronounced with carteolol incorporated into the colloidal carriers than with the commercial eye drops. Further, NC displayed a better effect than NP because the drug was entrapped in the oily core of the carrier, thus more readily available to the eye. The incorporation of the drug into nanocapsules produced a decline in the cardiovascular side effects in comparison with aqueous eye drops, thus showing that the undesired noncorneal absorption was reduced. In conclusion, colloidal suspension made of poly(ε-caprolactone) could offer a good opportunity for ophthalmic delivery of drugs.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Similar content being viewed by others

REFERENCES

  1. V. H. L. Lee and J. R. Robinson. Review: Topical ocular drug delivery. Recent developments and future challenges. J. Ocul. Pharm. 2:67–108 (1986).

    Google Scholar 

  2. S. C. Chang and V. H. L. Lee. Nasal and conjunctival contributions to the systemic absorption of topical timolol in the pigmented rabbit: Implications in the design and strategies to maximize the ratio of ocular to systemic absorption. J. Ocul. Pharm. 3:159–169 (1987).

    Google Scholar 

  3. D. Sirbat, C. Kholer, J. L. George, D. Mayeux, and J. P. Grilliat. Evaluation des effets systémiques cardiovasculaires et bronchiques d'un collyre β-bloquant. Ophtalmologie 2:213–218 (1988).

    Google Scholar 

  4. S. Ball. Congestive heart failure from betaxolol. Arch. Ophthalmol. 105:320 (1987).

    Google Scholar 

  5. K. Kishida and T. Otori. A quantitative study on the relationship between transcorneal permeability of drugs and their hydrophobicity. Jpn. J. Ophthalmol. 24:251–259 (1980).

    Google Scholar 

  6. L. Marchal-Heussler, H. Fessi, J. P. Devissaguet, M. Hoffman, and Ph. Maincent. Colloidal drug delivery systems for the eye. A comparison of the efficacy of three different polymers: Polyisobutylcyanoacrylate, polylactic-co-glycolic acid, polyepsilon-caprolactone. STP Pharma Sci. 2:98–104 (1992).

    Google Scholar 

  7. H. Fessi, F. Puisieux, J. P. Devissaguet, N. Ammoury, and S. Benita. Nanocapsules formation by interfacial polymer deposition following solvent displacement. Int. J. Pharm. 55:R1–R4 (1989).

    Google Scholar 

  8. P. Vareilles, P. Conquet, and J. C. Le Douarec. A method for the routine intraocular pressure (IOP) measurement in the rabbit: Range of IOP variations in this species. Exp. Eye Res. 24:269–282 (1977).

    Google Scholar 

  9. L. Marchal-Heussler, Ph. Maincent, M. Hoffman, J. Spittler, and P. Couvreur. Antiglaucomatous activity of betaxolol chlorhydrate sorbed onto different isobutylcyanoacrylate nanoparticle preparations. Int. J. Pharm. 58:115–122 (1990).

    Google Scholar 

  10. T. Harmia, J. Kreuter, P. Speiser, T. Boye, R. Gurny, and A. Kubis. Enhancement of the myotic response of rabbits with pilocarpine-loaded polybutylcyanoacrylate nanoparticles. Int. J. Pharm. 33:187–193 (1986).

    Google Scholar 

  11. P. Ashton, S. K. Podder, and V. H. L. Lee. Formulation influence on conjunctival penetration of four beta blockers in the pigmented rabbit: A comparison with corneal penetration. Pharm. Res. 9:1166–1174 (1991).

    Google Scholar 

  12. S. D. Troster, U. Muller, and J. Kreuter. Modification of the body distribution of poly(methylmethacrylate) nanoparticles in rats by coating with surfactants. Int. J. Pharm. 61:85–100 (1990).

    Google Scholar 

  13. N. Ammoury, H. Fessi, J. P. Devissaguet, F. Puisieux, and S. Benita. Physicochemical characterization of polymeric nanocapsules and in vitro release evaluation of indomethacin as a drug model. STP Pharma 5:647–651 (1989).

    Google Scholar 

  14. S. J. Ory, C. B. Hammond, S. G. Yancy, R. W. Hendren, and C. G. Pitt. The effect of a biodegradable contraceptive capsule (Capronor) containing levonorgestrel on gonadotropin, estrogen, and progesterone levels. Am. J. Obstet. Gynecol. 5:600–605 (1983).

    Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Laboratoire de Pharmacie Galénique, Biopharmacie et Pharmacie Hospitalière, Faculté de Pharmacie, 5 rue A. Lebrun, BP 403, 54001, Nancy Cedex, France

    Laurent Marchal-Heussler, Maurice Hoffman & Philippe Maincent

  2. Service d'Ophtalmologie, CHRU de Nancy-Brabois, 54511, Vandoeuvre-les-Nancy, France

    Daniel Sirbat

Authors
  1. Laurent Marchal-Heussler
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Daniel Sirbat
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. Maurice Hoffman
    View author publications

    You can also search for this author in PubMed Google Scholar

  4. Philippe Maincent
    View author publications

    You can also search for this author in PubMed Google Scholar

Rights and permissions

Reprints and permissions

About this article

Cite this article

Marchal-Heussler, L., Sirbat, D., Hoffman, M. et al. Poly(ε-Caprolactone) Nanocapsules in Carteolol Ophthalmic Delivery. Pharm Res 10, 386–390 (1993). https://doi.org/10.1023/A:1018936205485

Download citation

  • Issue Date:

  • DOI: https://doi.org/10.1023/A:1018936205485

Search

Navigation