Preparing simvastatin nanoparticles by a combination of pH-sensitive and timed-release approaches for the potential treatment of ulcerative colitis

In this study, an emulsion solvent evaporation method was used to produce Eudragit RL (ERL) nanoparticles (NPs) loaded with simvastatin (SIM) for the treatment of ulcerative colitis (UC). Accordingly, the effects of different formulation variables on the properties of NPs were evaluated using the Box-Behnken design. The optimized NPs were then coated by Eudragit FS30D (EFS30D). Drug release was studied in different physiological environments. Colitis was induced by 3% of acetic acid in rats, which received NPs of SIM (10 mg/kg/day), mesalazine (150 mg/kg/day), blank NPs and normal saline orally for 5 days. Macroscopic histopathological evaluation and biochemical analysis, including myeloperoxidase (MPO) activity and malondialdehyde (MDA) level in the colon tissues, were carried out in this study. The optimized SIM-ERL NPs showed the particle size of 182.48 ± 4.57 nm, the polydispersity index of 0.29 ± 0.12, the zeta potential of 26.45 ± 4.57 mV, drug loading % of 34.64 ± 0.48, the encapsulation efficiency % of 98.68 ± 0.69, and the release efficiency % of 35.78 ± 1.37. Coating the optimized NPs with EFS30D caused an increase in particle size and a decrease in the zeta potential of NPs. The optimized SIM-EFS30D/RL NPs improved the macroscopic and histopathological scores. Also, MPO activity and MDA level were reduced significantly by NPs, as compared to the control group. Therefore, this drug delivery system can be an alternative to the previous treatments of UC.

Medienart:

E-Artikel

Erscheinungsjahr:

2022

Erschienen:

2022

Enthalten in:

Zur Gesamtaufnahme - volume:37

Enthalten in:

Journal of biomaterials applications - 37(2022), 5 vom: 29. Nov., Seite 859-871

Sprache:

Englisch

Beteiligte Personen:

Fardafshari, Fereshteh [VerfasserIn]
Taymouri, Somayeh [VerfasserIn]
Minaiyan, Mohsen [VerfasserIn]
Tavakoli, Naser [VerfasserIn]

Links:

Volltext

Themen:

25086-15-1
AGG2FN16EV
Acetic acid-induced colitis
Drug Carriers
Eudragit FS30D
Eudragit RL
Experimental design
Journal Article
Methylmethacrylate-methacrylic acid copolymer
Nanoparticles
Research Support, Non-U.S. Gov't
Simvastatin

Anmerkungen:

Date Completed 01.11.2022

Date Revised 14.11.2022

published: Print-Electronic

Citation Status MEDLINE

doi:

10.1177/08853282221122907

funding:

Förderinstitution / Projekttitel:

PPN (Katalog-ID):

NLM345174887