title: Development and evaluation of decorated aceclofenac nanocrystals.
abstract: This study was aimed at achieving enhanced solubility of aceclofenac (ACF) in nanocrystaline forms (ACF-NC) and evaluating the effects of ACF-NC on cell viability. Decorated ACF-NC were prepared by nano-precipitation with stabilizers. Three kinds of stabilizers were investigated: Tween 80, Poloxamer 407, and PEG 6000. The crystal structure and morphology of ACF-NC were characterized by field emission scanning electron microscopy (FE-SEM) and differential scanning calorimetry (DSC). The solubility of ACF-NC and ACF (pure) was evaluated in different media (pH 1.2 and pH 6.8 buffers and distilled water [DW]). A drug release study was performed in PBS for 24h. Cell viability was evaluated for 24h using a human colon cancer cell-line (HCT-116) and a human breast cancer cell-line (MCF-7). Decorated ACF-NC with a mean size of 725nm were successfully prepared. The solubility of the decorated ACF-NC were 4-7 times higher than that of ACF in DW and pH 6.8 buffer. A peak shift from 153.1°C to 150.5-151.0°C was observed in the DSC thermogram of decorated ACF-NC versus ACF. In terms of drug release, there was an initial burst in decorated ACF-NC within 1h followed by slow release for up to 4h. Decorated ACF-NC exhibited viability approximately 63.9% of HCT-116 cells and also showed viability in 58.3% of MCF-7 cells at 15μg/mL of drug concentration. In conclusion, decorated ACF-NC proved to be a promising approach for enhancing drug solubility and cytotoxicity.
authors.affiliation: College of Pharmacy, Ajou University, Suwon-si, Gyounggi-do 443-749, Republic of Korea.
authors.forename: Jeong-Joo
authors.initials: JJ
authors.lastname: Park
authors.affiliation: College of Pharmacy, Ajou University, Suwon-si, Gyounggi-do 443-749, Republic of Korea.
authors.forename: Nilesh
authors.initials: N
authors.lastname: Meghani
authors.affiliation: College of Pharmacy, Ajou University, Suwon-si, Gyounggi-do 443-749, Republic of Korea. Electronic address: c34281@gmail.com.
authors.forename: Jin-Seok
authors.initials: JS
authors.lastname: Choi
authors.affiliation: College of Pharmacy, Ajou University, Suwon-si, Gyounggi-do 443-749, Republic of Korea. Electronic address: beomjinlee@gmail.com.
authors.forename: Beom-Jin
authors.initials: BJ
authors.lastname: Lee
mesh_terms: D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D002152:Calorimetry, Differential Scanning; D002470:Cell Survival / Q000187:drug effects; D004008:Diclofenac / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004339:Drug Compounding / Q000379:methods*; D065546:Drug Liberation; D045325:HCT116 Cells; D006801:Humans; D006863:Hydrogen-Ion Concentration; D061986:MCF-7 Cells; D008855:Microscopy, Electron, Scanning; D015394:Molecular Structure; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D020442:Poloxamer / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry; D011136:Polysorbates / Q000737:chemistry; D012995:Solubility
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D011136:Polysorbates; D020442:Poloxamer; D004008:Diclofenac; C000595215:Polyethylene Glycol 6000; D011092:Polyethylene Glycols; C056498:aceclofenac
keywords: Aceclofenac (ACF); Cell viability; Drug release; Nanocrystals (NC); Solubility