In vitro testing of thiolated poly(aspartic acid) from ophthalmic formulation aspects

Drug Dev Ind Pharm. 2016 Aug;42(8):1241-6. doi: 10.3109/03639045.2015.1118497. Epub 2015 Dec 7.

Abstract

Ocular drug delivery formulations must meet anatomical, biopharmaceutical, patient-driven and regulatory requirements. Mucoadhesive polymers can serve as a better alternative to currently available ophthalmic formulations by providing improved bioavailability. If all requirements are addressed, a polymeric formulation resembling the tear film of the eye might be the best solution. The optimum formulation must not have high osmotic activity, should provide appropriate surface tension, pH and refractive index, must be non-toxic and should be transparent and mucoadhesive. We would like to highlight the importance of in vitro polymer testing from a pharmaceutical aspect. We, therefore, carried out physical-chemical investigations to verify the suitability of certain systems for ophthalmic formulations. In this work, in situ gelling, mucoadhesive thiolated poly(aspartic acid)s were tested from ophthalmic formulation aspects. The results of preformulation measurements indicate that these polymers can be used as potential carriers in ophthalmic drug delivery.

Keywords: Cytotoxicity; mucoadhesion; ocular drug delivery; pharmaceutical preformulation; rheology; thiolated polymer.

MeSH terms

  • Adhesiveness
  • Animals
  • Aspartic Acid / chemistry*
  • Aspartic Acid / metabolism
  • Biological Availability
  • Cell Line
  • Chemistry, Pharmaceutical / methods
  • Drug Carriers / chemistry
  • Drug Delivery Systems / methods
  • Eye / metabolism*
  • Gels / chemistry
  • Ophthalmic Solutions / chemistry*
  • Ophthalmic Solutions / metabolism
  • Polymers / chemistry
  • Rabbits
  • Rheology / methods
  • Sulfhydryl Compounds / chemistry*
  • Sulfhydryl Compounds / metabolism

Substances

  • Drug Carriers
  • Gels
  • Ophthalmic Solutions
  • Polymers
  • Sulfhydryl Compounds
  • Aspartic Acid