Influence of cyclodextrins on the in vitro corneal permeability and in vivo ocular distribution of thalidomide
| Autor: | Sigrid Keipert, Martina Müller, Christian Hartmann, Burkhard Siefert, Uwe Pleyer |
|---|---|
| Rok vydání: | 1999 |
| Předmět: |
Male
medicine.medical_specialty Time Factors medicine.medical_treatment Excipient Biological Availability Iris Angiogenesis Inhibitors Pharmacology In Vitro Techniques Permeability Aqueous Humor Cornea Pharmacokinetics In vivo medicine Animals Pharmacology (medical) Drug Interactions Cyclodextrins Chemistry Ciliary Body Eye drop In vitro Surgery Bioavailability Thalidomide Vitreous Body Ophthalmology medicine.anatomical_structure Cattle Rabbits Ophthalmic Solutions Conjunctiva Sclera medicine.drug |
| Zdroj: | Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics. 15(5) |
| ISSN: | 1080-7683 |
| Popis: | The aim of the present study has been to develop aqueous Thalidomide (THA) eye drops in order to minimize systemic side effects and to improve bioavailability following topical application. Cyclodextrins (CDs), suitable vehicles to improve aqueous solubility of THA, were evaluated with regard to their ability to influence in vitro corneal permeability of THA. Additionally, rabbit eyes received either THA-suspension (0.04%) (THA-SP) or THA (0.04%)/hydroxypropyl-beta-cyclodextrin (HP-beta-CD) (12.5%) solution (THA-CD). In vitro corneal permeation studies demonstrated that the absolute amount of THA permeated could not be increased by means of CDs. The percentile release of THA was extensively decreased using saturated THA/CD solutions. Following loading doses of either THA-CD or THA-SP onto the rabbit eye, significantly increased aqueous humor levels were obtained for THA-CD 30 min (THA-CD:THA-SP=4.6:1) and 60 min (THA-CD:THA-SP=3.1:1) post instillation (p0.05). In the iris-ciliary body, significantly increased THA levels were obtained using THA suspension (THA-CD(60 min):THA-SP(60 min)=1:6.1) (p0.05). In the cornea, conjunctiva, vitreous and sclera, differences between the THA tissue levels were not statistically significant. Cyclodextrins might be a useful tool to formulate aqueous THA eye drop solutions and modify intraocular drug bioavailability. |
| Databáze: | OpenAIRE |
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