Optimization of nimesulide-loaded solid lipid nanoparticles (SLN) by factorial design, release profile and cytotoxicity in human Colon adenocarcinoma cell line

• Type: Article in International Scientific Journal
• Date: 2019

Authors

Campos, JR (Author) Other; Fernandes, AR (Author) Other; Sousa, R (Author) Other; Fangueiro, JF (Author) Other; Boonme, P (Author) Other; Garcia, ML (Author) Other; Silva, AM (Author) Other; Naveros, BC (Author) Other; Souto, EB (Author) Other

Journal

Title: Pharmaceutical Development and Technology

Vol. 24

Pages: 616-622

ISSN: 1083-7450

Publisher: Taylor & Francis

Indexing

ISI Web of Knowledge - 27 Citations

Scopus - 24 Citations

Other information

Authenticus ID: P-00Q-3J3

DOI: 10.1080/10837450.2018.1549075

Abstract (EN): The aim of this work is development of a nontoxic, long-term stable solid lipid nanoparticles (SLN) formulation for the loading of Nimesulide (NiM) by a 2(2) factorial design. The optimized formulation was composed of 10 wt% of glyceryl behenate and 2.5 wt% of poloxamer 188. Immediately after production, Z-Ave of NiM-SLN was 166.1 +/- 0.114 nm, with a polydispersity index (PI) of 0.171 +/- 0051 and zeta potential nearly neutral (-3.10 +/- 0.166 mV). A slight increase of Z-Ave was recorded for NiM-SLN stored at 25 degrees C for a period of 15 days, whereas at 4 degrees C particles kept size within similar range. Long-term stability was monitored using TurbiscanLab (R), showing a high stability of the nanoparticles with variations in the backscattering profiles below 10%. The release profile of NiM-SLN followed a sustained pattern with ca. 30% of drug released up to 24 h. Empty-SLN and NiM-SLN were nontoxic after exposing Caco-2 cells to the highest concentration (100 mu g/mL) up to 48 hours (cell viability higher than 80%). NiM-SLN were lyophilized using different cryoprotectants, producing particles of 463.1 +/- 36.63 nm (PI 0.491 +/- 0.027) with 5% trehalose. Solid character of NiM-SLN was confirmed by DSC, recording a recrystallization index of 83% for NiM-SLN and of 74% for lyophilized SLN.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 7