Abstract
The aim of this work was to evaluate the effectiveness of neat chitosan (CS) and its derivatives with 2-acrylamido-2-methyl-1-propanesulfonic acid (AAMPS) and [2-(methacryloyloxy)ethyl]dimethyl-(3-sulfopropyl)ammonium hydroxide (MEDSP) as appropriate nanocarriers for the simultaneous ocular administration of dexamethasone sodium phosphate (DxP) and chloramphenicol (CHL). The derivatives CS-AAMPS and CS-MEDSP have been synthesized by free-radical polymerization and their structure has been proved by Fourier-Transformed Infrared Spectroscopy (FT-IR) spectroscopy. Both derivatives exhibited low cytotoxicity, enhanced mucoadhesive properties and antimicrobial activity against Staphylococcus aureus (S.aureus) and Escherichia coli (E. coli). Encapsulation was performed via ionic crosslinking gelation using sodium tripolyphosphate (TPP) as the crosslinking agent. Dynamic light scattering measurements (DLS) showed that the prepared nanoparticles had bimodal distribution and sizes ranging from 50–200 nm and 300–800 nm. Drugs were encapsulated in their crystalline (CHL) or amorphous (DexSP) form inside nanoparticles and their release rate was dependent on the used polymer. The CHL dissolution rate was substantially enhanced compared to the neat drug and the release time was extended up to 7 days. The release rate of DexSP was much faster than that of CHL and was prolonged up to 3 days. Drug release modeling unveiled that diffusion is the main release mechanism for both drugs. Both prepared derivatives and their drug-loaded nanoparticles could be used for extended and simultaneous ocular release formulations of DexSP and CHL drugs.
Highlights
Most of the common eye diseases are treated with eye drops where drugs have been dissolved, since they are the simplest, safe and easy-to-use formulations [1]
Taking all that has previously been discussed into account, the aim of the present work is to enhance the solubility of CHL and to prepare sustained release drug formulations with enhanced mucoadhesion properties for both CHL and dexamethasone sodium phosphate (DexSP) drugs
CS derivatives were synthesized by free-radical polymerization
Summary
Most of the common eye diseases are treated with eye drops where drugs have been dissolved, since they are the simplest, safe and easy-to-use formulations [1]. They must be able to adhere to the mucosa This ability arises from their property to interact with the mucosal membrane by several ways, including physical bonding, such as interfusion or interpenetration into the mucus layer, or secondary chemical interactions, mainly ionic interactions or hydrogen bond formation. Regarding the latter, the selected polymers must contain appropriate reactive groups, such as carboxyl (–COOH), amino (–NH2), hydroxyl (–OH), sulfate (–SO3H), etc
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
