PMID- 23866721 OWN - NLM STAT- MEDLINE DCOM- 20150312 LR - 20220408 IS - 1560-8115 (Print) IS - 2008-2231 (Electronic) IS - 1560-8115 (Linking) VI - 21 IP - 1 DP - 2013 Jul 17 TI - Surface modification of PLGA nanoparticles via human serum albumin conjugation for controlled delivery of docetaxel. PG - 58 LID - 10.1186/2008-2231-21-58 [doi] AB - BACKGROUND: Poly lactic-co-glycolic acid (PLGA) based nanoparticles are considered to be a promising drug carrier in tumor targeting but suffer from the high level of opsonization by reticuloendothelial system due to their hydrophobic structure. As a result surface modification of these nanoparticles has been widely studied as an essential step in their development. Among various surface modifications, human serum albumin (HSA) possesses advantages including small size, hydrophilic surface and accumulation in leaky vasculature of tumors through passive targeting and a probable active transport into tumor tissues. METHODS: PLGA nanoparticles of docetaxel were prepared by emulsification evaporation method and were surface conjugated with human serum albumin. Fourier transform infrared spectrum was used to confirm the conjugation reaction where nuclear magnetic resonance was utilized for conjugation ratio determination. In addition, transmission electron microscopy showed two different contrast media in conjugated nanoparticles. Furthermore, cytotoxicity of free docetaxel, unconjugated and conjugated PLGA nanoparticles was studied in HepG2 cells. RESULTS: Size, zeta potential and drug loading of PLGA nanoparticles were about 199 nm, -11.07 mV, and 4%, respectively where size, zeta potential and drug loading of conjugated nanoparticles were found to be 204 nm, -5.6 mV and 3.6% respectively. Conjugated nanoparticles represented a three-phasic release pattern with a 20% burst effect for docetaxel on the first day. Cytotoxicity experiment showed that the IC50 of HSA conjugated PLGA nanoparticles (5.4 mug) was significantly lower than both free docetaxel (20.2 mug) and unconjugated PLGA nanoparticles (6.2 mug). CONCLUSION: In conclusion surface modification of PLGA nanoparticles through HSA conjugation results in more cytotoxicity against tumor cell lines compared with free docetaxel and unconjugated PLGA nanoparticles. Albumin conjugated PLGA nanoparticles may represent a promising drug delivery system in cancer therapy. FAU - Manoochehri, Saeed AU - Manoochehri S FAU - Darvishi, Behrad AU - Darvishi B FAU - Kamalinia, Golnaz AU - Kamalinia G FAU - Amini, Mohsen AU - Amini M FAU - Fallah, Mahdieh AU - Fallah M FAU - Ostad, Seyed Naser AU - Ostad SN FAU - Atyabi, Fatemeh AU - Atyabi F FAU - Dinarvand, Rassoul AU - Dinarvand R LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't DEP - 20130717 PL - Switzerland TA - Daru JT - Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences JID - 101125969 RN - 0 (Serum Albumin) RN - 0 (Taxoids) RN - 15H5577CQD (Docetaxel) RN - 1SIA8062RS (Polylactic Acid-Polyglycolic Acid Copolymer) RN - 26009-03-0 (Polyglycolic Acid) RN - 33X04XA5AT (Lactic Acid) SB - IM MH - Cell Survival/drug effects MH - Docetaxel MH - Hep G2 Cells MH - Humans MH - Lactic Acid/*chemistry MH - Nanoparticles/*chemistry MH - Particle Size MH - Polyglycolic Acid/*chemistry MH - Polylactic Acid-Polyglycolic Acid Copolymer MH - Serum Albumin/*chemistry MH - Spectroscopy, Fourier Transform Infrared MH - Taxoids/*pharmacology PMC - PMC3720529 EDAT- 2013/07/23 06:00 MHDA- 2015/03/13 06:00 PMCR- 2013/07/17 CRDT- 2013/07/23 06:00 PHST- 2013/04/22 00:00 [received] PHST- 2013/07/15 00:00 [accepted] PHST- 2013/07/23 06:00 [entrez] PHST- 2013/07/23 06:00 [pubmed] PHST- 2015/03/13 06:00 [medline] PHST- 2013/07/17 00:00 [pmc-release] AID - 2008-2231-21-58 [pii] AID - 10.1186/2008-2231-21-58 [doi] PST - epublish SO - Daru. 2013 Jul 17;21(1):58. doi: 10.1186/2008-2231-21-58.