Incorporation of ion exchange functionalized-montmorillonite into solid lipid nanoparticles with low irritation enhances drug bioavailability for glaucoma treatment

Autor: Zhufen Lv, Huamei Li, Hanyu Liu, Yanzhong Chen, Dongzhi Hou, Pan Yufang, Ilva D. Rupenthal, Fan Yang, Xinyue Han, Shuo Liu, Qineng Ping, Yawen Zhao
Jazyk: angličtina
Rok vydání: 2020
Předmět:
immortalized human cornea epithelial cells (ihcecs)
Pharmaceutical Science
Biocompatible Materials
02 engineering and technology
medicine.disease_cause
030226 pharmacology & pharmacy
Cornea
chemistry.chemical_compound
0302 clinical medicine
Drug Stability
Drug Carriers
Ion exchange
General Medicine
021001 nanoscience & nanotechnology
Bentonite
Rabbits
betaxolol hydrochloride (bh)
Irritation
0210 nano-technology
montmorillonite (mt)
Biocompatibility
Cell Survival
Surface Properties
Sonication
Drug Compounding
Biological Availability
RM1-950
Betaxolol Hydrochloride
Cell Line
Aqueous Humor
03 medical and health sciences
Solid lipid nanoparticle
medicine
Animals
Humans
intraocular pressure (iop)
Particle Size
Intraocular Pressure
solid lipid nanoparticles (slns)
Original Paper
Epithelial Cells
Glaucoma
Bioavailability
Betaxolol
Disease Models
Animal
Drug Liberation
Montmorillonite
chemistry
Nanoparticles
Therapeutics. Pharmacology
Nuclear chemistry
Zdroj: Drug Delivery, Vol 27, Iss 1, Pp 652-661 (2020)
Drug Delivery
ISSN: 1521-0464
1071-7544
Popis: Montmorillonite-loaded solid lipid nanoparticles with good biocompatibility, using Betaxolol hydrochloride as model drug, were prepared by the melt-emulsion sonication and low temperature-solidification methods and drug bioavailability was significantly improved in this paper for the first time to application to the eye. The appropriate physical characteristics were showed, such as the mean particle size, Zeta potential, osmotic pressure, pH values, entrapping efficiency (EE%) and drug content (DC%), all showed well suited for possible ocular application. In vitro release experiment indicated that this novel system could continuously release 57.83% drugs within 12 h owing to the dual drug controlled-release effect that was achieved by ion-exchange feature of montmorillonite and structure of solid lipid nanoparticles. Low irritability and good compatibility of nanoparticles were proved by both CAM-TBS test and cytotoxicity experiment. We first discovered from the results of Rose Bengal experiment that the hydrophilicity of the drug-loaded nanoparticles surface was increased during the loading and releasing of the hydrophilic drug, which could contribute to prolong the ocular surface retention time of drug in the biological interface membrane of tear-film/cornea. The results of in vivo pharmacokinetic and pharmacodynamics studies further confirmed that increased hydrophilicity of nanoparticles surface help to improve the bioavailability of the drug and reduce intraocular pressure during administration. The results suggested this novel drug delivery system could be potentially used as an in situ drug controlled-release system for ophthalmic delivery to enhance the bioavailability and efficacy.
Databáze: OpenAIRE
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