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Carboxymethyl Cellulose-Coated Tacrolimus Nonspherical Microcrystals for Improved Therapeutic Efficacy of Dry Eye
- Source :
- Macromolecular bioscience. 20(7)
- Publication Year :
- 2020
-
Abstract
- Dry eye (DE) is a highly prevalent ocular surface disease which affects the quality of life and results in low working efficiency. Frequent instillation is required due to low bioavailability of conventional eye drops. The aim of this study is to develop a novel formulation of tacrolimus (TAC), routinely prescribed for DE, by combination of the microcrystal technology and layer-by-layer assembly. First, nonspherical tacrolimus microcrystals (TAC MCs) are synthesized by antisolvent-induced precipitation. These TAC MCs are modified by alternate deposition of poly(allylamine hydrochloride) (PAH) and carboxymethyl cellulose (CMC) subsequently to obtain CMC-coated TAC MCs (TAC-(PAH/CMC)3 ). The resultant formulations are evaluated in vivo in a mouse DE model induced by an intelligently controlled environmental system. Compared with commercially available TAC eye drops and the TAC MCs counterpart, TAC-(PAH/CMC)3 exhibits superior therapeutic performance with reduced drug instillation frequency, which is attributed to the nonspherical geometry of MCs, the lubricant, mucoadhesive effect of CMC, and the anti-inflammatory function of TAC. Therefore, TAC-(PAH/CMC)3 represents a better option for the management of DE.
- Subjects :
- Polymers and Plastics
Hydrochloride
Interleukin-1beta
chemical and pharmacologic phenomena
Bioengineering
02 engineering and technology
010402 general chemistry
01 natural sciences
Tacrolimus
Allylamine
Biomaterials
chemistry.chemical_compound
stomatognathic system
In vivo
Materials Chemistry
medicine
Polyamines
Animals
Environmental systems
Inflammation
Chromatography
Ocular surface disease
Epithelium, Corneal
021001 nanoscience & nanotechnology
0104 chemical sciences
Carboxymethyl cellulose
Bioavailability
Mice, Inbred C57BL
stomatognathic diseases
Disease Models, Animal
Treatment Outcome
chemistry
Matrix Metalloproteinase 9
Carboxymethylcellulose Sodium
Tears
Dry Eye Syndromes
Female
Goblet Cells
0210 nano-technology
Crystallization
Biotechnology
medicine.drug
Subjects
Details
- ISSN :
- 16165195
- Volume :
- 20
- Issue :
- 7
- Database :
- OpenAIRE
- Journal :
- Macromolecular bioscience
- Accession number :
- edsair.doi.dedup.....3ba5cfaba9c872dc0ec033c22e2306a2