ABSTRACT
AIM: This work aimed to design and characterize cross-linked hyaluronic acid-itaconic acid films loaded with acetazolamide-hydroxypropyl ß cyclodextrin-triethanolamine complexes. MATERIALS & METHODS: Films were cross-linked with itaconic acid and poly(ethyleneglycol)-diglycidylether. Biopharmaceutical properties were assessed by evaluating in vitro drug release rate, biocompatibility in a human corneal epithelial cell line, bioadhesiveness with pig gastric mucin, in vivo bioadhesion and efficacy. RESULTS: Showed good mechanical properties and oxygen permeability. Proliferation rate of corneal cells was affected by highest acetazolamide concentration. Bioadhesive interaction exhibited a water movement from pig mucin to the film; in vivo experiments showed strong bioadhesion for 8 h and hypotensive effect for almost 20 h. CONCLUSION: Experimental set showed promising performance and encouraged future studies to optimize formulation. [Formula: see text].
Subject(s)
2-Hydroxypropyl-beta-cyclodextrin/administration & dosage , Acetazolamide/administration & dosage , Ethanolamines/administration & dosage , Glaucoma/drug therapy , Hyaluronic Acid/chemistry , 2-Hydroxypropyl-beta-cyclodextrin/pharmacokinetics , Acetazolamide/pharmacokinetics , Administration, Ophthalmic , Animals , Cell Line , Cross-Linking Reagents/chemistry , Drug Combinations , Drug Liberation , Epithelial Cells , Ethanolamines/pharmacokinetics , Humans , Male , Models, Animal , RabbitsABSTRACT
New hyaluronic acid-itaconic acid films were synthesized as potential materials with biomedical applications. In this work, we explored the homogeneous cross-linking reactions of hyaluronic acid using glutaraldehyde in the presence of itaconic acid and triacetin as plasticizers. Biomechanical properties were assessed in terms of stability by measuring swelling in aqueous environments, investigating wettability using contact angle tests, and evaluating bioadhesive performance. The ductility of the materials was evaluated through stress-strain measurements and the morphology was explored by scanning electron microscopy. The results show that the incorporation of itaconic acid improved most of the desirable properties, increasing adhesiveness and reducing wettability and swelling. The use of triacetin enhanced the strength, bioadhesiveness, and ductility of the material.
ABSTRACT
Obtaining successful ocular formulations able to support an efficient drug concentration at the target tissue for an appropriate period of time is an interesting challenge for modern pharmaceutical technology. In this sense, nanotechnology is one of the available strategies to obtain a drug carrier system that allows access to different compartments of the eye in order to deliver drugs to the desired site. Biodegradable polymers such as polysaccharides are promising biomaterials for the production of biocompatible and biodegradable nanocarriers (NCs). Different types of polysaccharide NCs are capable of improving the transport of drugs after ocular application and they can be either polysaccharide-matrix carriers or polysaccharide-coated carriers, depending on whether polysaccharide is used as a matrix or as a coating, respectively. This review focuses on recent advances achieved by polysaccharide-based NCs for the treatment of ocular disorders.
