SN38 loaded nanostructured lipid carriers (NLCs); preparation and in vitro evaluations against glioblastoma

• Published in: Journal of materials science. Materials in medicine 2021-07, Vol.32 (7), p.78, Article 78
• Main Authors: Shirazi, Ali Sabouri, Varshochian, Reyhaneh, Rezaei, Mahsa, Ardakani, Yalda Hosseinzadeh, Dinarvand, Rassoul
• Format: Article
• Language: English
• Subjects: Biomaterials; Biomedical Engineering and Bioengineering; Biomedical materials; Brain cancer; Calorimetry, Differential Scanning; Cell Line, Tumor; Ceramics; Chemistry and Materials Science; Chemistry, Pharmaceutical - methods; Composites; Confocal microscopy; Cytotoxicity; Delivery Systems; Drug Carriers; Drug Compounding; Drug Delivery Systems; Drug Liberation; Drug Screening Assays, Antitumor; Emulsification; Entrapment; Evaporation; Excipients; Glass; Glioblastoma; Glioblastoma - drug therapy; Humans; Hydrogen-Ion Concentration; Hydrophobic and Hydrophilic Interactions; In Vitro Techniques; Irinotecan; Irinotecan - pharmacology; Lipids; Lipids - chemistry; Materials Science; Metabolites; Microscopy, Confocal; Nanoparticles - chemistry; Nanostructure; Nanostructures - chemistry; Natural Materials; Particle Size; Particle size distribution; Polymer Sciences; Regenerative Medicine/Tissue Engineering; Size distribution; Solubility; Solvents; Solvents - chemistry; Surfaces and Interfaces; Tetrazolium Salts - chemistry; Thiazoles - chemistry; Thin Films; Toxicity
• ISSN: 0957-4530; 1573-4838
• DOI: 10.1007/s10856-021-06538-2

SN38 is the active metabolite of irinotecan with 1000-fold greater cytotoxicity compared to the parent drug. Despite the potential, its application as a drug is still seriously limited due to its stability concerns and low solubility in acceptable pharmaceutical solvents. To address these drawbacks here nanostructured lipid carrier (NLC) containing SN38 was prepared and its cytotoxicity against U87MG glioblastoma cell line was investigated. The formulations were prepared using hot ultrasonication and solvent evaporation/emulsification methods. NLCs with a mean size of 140 nm and particle size distribution (PDI) of 0.25 were obtained. The average loading efficiency was 9.5% and its entrapment efficiency was 81%. In order to obtain an accurate determination of released amount of SN38 a novel medium and extraction method was designed, which lead to an appropriate in vitro release profile of the drug from the prepared NLCs. The MTT test results revealed the significant higher cytotoxicity of NLCs on U87MG human glioblastoma cell line compared with the free drug. The confocal microscopy images confirmed the proper penetration of the nanostructures into the cells within the first 4 h. Consequently, the results indicated promising potentials of the prepared NLCs as a novel treatment for glioblastoma.