Chitosan temperature-sensitive gel loaded with drug microspheres has excellent effectiveness, biocompatibility and safety as an ophthalmic drug delivery system

نویسندگان

  • Xiaoying Kong
  • Wenhua Xu
  • Cuiping Zhang
  • Wei Kong
چکیده

In the present study, a temperature-sensitive gel composed of chitosan, carboxymethyl chitosan and glycerophosphate was prepared and loaded with chitosan microspheres encapsulating levofloxacin. The bioavailability of levofloxacin and the safety of this novel opthalmic drug delivery formulation were evaluated. Levofloxacin chitosan microspheres were prepared using the ionic gelation method, and the particle size and entrapment rate were determined. The morphology of the microspheres was observed by scanning electron microscopy. The pH and zeta potential were measured. The in vitro release of levofloxacin by the chitosan temperature-sensitive gel loaded with drug microspheres was determined using spectrophotometry. The eye retention time of the chitosan temperature-sensitive gel was calculated using a fluorescein sodium test. To assess the bioavailability and safety of the chitosan temperature-sensitive gel, a cell compatibility test, a cytotoxicity test and skin irritation test were performed. The entrapment rate of levofloxacin in the chitosan microspheres was determined to be 26.5%. The levofloxacin chitosan microspheres that were formed by chitosan and sodium tripolyphosphate were identified to be suitable for use in an ophthalmic particle dispersion system based on their physical and chemical properties. The pH of the levofloxacin chitosan microsphere suspension was 5.87±0.04, the average particle diameter was 2,452±342 nm, the polydispersity index was 0.168±0.028 and the ζ potential was 28.62±1.7 mV. The chitosan temperature-sensitive gel carrying microspheres loaded with drug prevented drug burst release at the initial stage and facilitated the slow release of the drug later on. Furthermore, this delivery system markedly prolonged the contact duration of levofloxacin with the eye. The chitosan temperature-sensitive hydrogel was safe and provided a good bioavailability of the drug. The results revealed that the chitosan temperature-sensitive gel had a cytotoxicity of grade 0, and no erythematous response was observed during the entire course of the skin irritation test. The present study provided a basis for the future development of the chitosan-based temperature-sensitive hydrogel in ophthalmic drug delivery.

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Preparation and Characterization of Theophylline-Chitosan Beads as an Aapproach to Colon Delivery

Chitosan with excellent biodegradable and biocompatible characteristics has received attention as an oral drug delivery vehicle for controlled-release formulations. In this study an enteric-coated capsule containing theophylline-chitosan beads based on 23 factorial designs was prepared as a colon drug delivery system. The theophylline-chitosan gel beads were formulated by adding the drug-contai...

متن کامل

Preparation and Characterization of Theophylline-Chitosan Beads as an Aapproach to Colon Delivery

Chitosan with excellent biodegradable and biocompatible characteristics has received attention as an oral drug delivery vehicle for controlled-release formulations. In this study an enteric-coated capsule containing theophylline-chitosan beads based on 23 factorial designs was prepared as a colon drug delivery system. The theophylline-chitosan gel beads were formulated by adding the drug-contai...

متن کامل

Exploring the potential of complex-vesicle based niosomal ocular system loaded with azithromycin: Development of in situ gel and ex vivo characterization

Abstract Bacterial conjunctivitis characterized as pink eye referred as an inflammation of an eye caused by the enlargement of blood vessels present in conjunctiva, resulting in a red or bloodshot appearance of the eyes. Topical ocular delivery is found to be useful in treating conjunctivitis, but to maintain an effective drug concentration at a site of action in order to achieve desired pha...

متن کامل

Preparation, Characterization and Evaluation of Drug Release Properties of Simvastatin-loaded PLGA Microspheres

Microspheres formulated from poly (D,L-lactic-co-glycolide) (PLGA), a biodegradable polymer, have been extensively evaluated as a drug delivery system. In this study, the preparation, characterization and drug release properties of the PLGA microspheres were evaluated. Simvastatin (SIM)-loaded PLGA microspheres were prepared by oil-in-water emulsion/solvent evaporation method. The microspheres ...

متن کامل

Preparation, Characterization and Evaluation of Drug Release Properties of Simvastatin-loaded PLGA Microspheres

Microspheres formulated from poly (D,L-lactic-co-glycolide) (PLGA), a biodegradable polymer, have been extensively evaluated as a drug delivery system. In this study, the preparation, characterization and drug release properties of the PLGA microspheres were evaluated. Simvastatin (SIM)-loaded PLGA microspheres were prepared by oil-in-water emulsion/solvent evaporation method. The microspheres ...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

عنوان ژورنال:

دوره 15  شماره 

صفحات  -

تاریخ انتشار 2018