Development of prednisolone-containing eye drop formulations by cyclodextrin complexation and antimicrobial, mucoadhesive biopolymer

Abstract

PurposeThe formulation of topical ophthalmic products with appropriate therapeutic effect and patient compliance is a major challenge. To increase the efficiency of the ocular delivery of the drug, the enhancement of water solubility and the contact time of the drug on the surface of the cornea are necessary. In this work, prednisolone (PR)-containing eye drops were formulated with antimicrobial, mucoadhesive biopolymer and PR–cyclodextrin inclusion complex. This approach can be used for the development of innovative ophthalmic formulations.Materials and methodsAfter adjusting the optimal physiological parameters, the amount of the required cyclodextrin for the highest penetration of PR was determined by dialysis membrane diffusion study. The viscosity, surface tension and mucoadhesion of the eye drops were measured. The microbiological effectiveness of zinc-hyaluronate (ZnHA) was investigated by a standard method of the European Pharmacopoeia.ResultsIn this case, no significant difference of surface tension was measured in products with different amounts of cyclodextrin. According to the results of the tensile test, ZnHA as a mucoadhesive biopolymer improves the mucoadhesion of ophthalmic products. The antimicrobial stability of formulations preserved by ZnHA meets requirement B of the European Pharmacopoeia.ConclusionIt can be stated that the innovative PR-containing compositions are suitable for producing mucoadhesive, properly preserved aqueous ophthalmic solutions with increased bioavailability attributes.

A Potential Alternative Orodispersible Formulation to Prednisolone Sodium Phosphate Orally Disintegrating Tablets

“…This is due to its availability as ODT (Orapred ODT ® ) and to its various therapeutic indications, in both geriatric and pediatric population, to treat several health conditions such as severe allergies, breathing difficulties (e.g., asthma and croup), immune system disorders (e.g., systemic lupus erythematosus), hematological disorders (e.g., hemolytic anemia and chronic lymphocytic leukemia), and rheumatoid arthritis [ 14 ].Furthermore, PSP was also suitable to be loaded onto multiple dosage forms. It was used in the salt form due to its improved solubility and therefore, oral bioavailability [ 15 ]. PSP requires dosages starting from 1 mg/day up to a maximum dose of 60 mg/day in children [ 14 ], and fast disintegrating oral drug delivery systems show promise as age-appropriate formulation platforms.…”

Anti-Tumor Efficiency of Perillylalcohol/β-Cyclodextrin Inclusion Complexes in a Sarcoma S180-Induced Mice Model

“…Besides, it modifies the drug release profile [ 26 ]. In the present work, β-CD has been selected on the basis of reports successfully describing the synthesis of inclusion complexes [ 27 , 28 , 29 ]. Advantages of complexing compounds with β-CDs are described for non-polar natural products, such as terpenes and essential oils [ 30 ].…”

New Approach in Ocular Drug Delivery: In vitro and ex vivo Investigation of Cyclodextrin-Containing, Mucoadhesive Eye Drop Formulations

“…The physiological parameters (surface tension, pH, osmolality) were set with optimized mucoadhesive, rheological, and preservative attributes. 12 The aim of this study was to continue and complete the research by investigating the cytotoxicity and API permeability of the formulation on an in vitro human corneal cell line and ex vivo, porcine cornea model.…”

“…Eye drops with prednisolone (PR), prednisoloneacetate, dexamethasone, fluorometholone, and fluocinolone are licensed worldwide. [11][12][13] PR is mostly used in acetate-form as a suspension; however, it is more watersoluble than the base form. Problems of suspension formulations are well known.…”

“…Increasing the efficiency could be possible with a selection of appropriate additives. 12 The efficiency can be increased by optimization of the amount of dissolved API molecules at the site of drug absorption. By using cyclodextrin (CD) derivatives the solubility of drug can be increased, therefore a solution as a dosage form can be prepared with minimal irritative effect and optimal permeation of API.…”