title: Sustained release of piroxicam from solid lipid nanoparticle as an effective anti-inflammatory therapeutics in vivo.
abstract: This study aims to investigate the solid lipid nanoparticle (SLN) as a novel vehicle for the sustained release and transdermal delivery of piroxicam, as well as to determine the anti-inflammation effect of piroxicam-loaded SLN. SLN formulation was optimized and the particle size, polydispersity index, zeta potential (ZP), encapsulation efficiency, drug release, and morphological properties were characterized. The transdermal efficiency and mechanism of the piroxicam-loaded SLNs were investigated in vitro. With the inflammation induced edema model in rat, the anti-inflammatory efficiency of piroxicam-enriched SLNs (Pir-SLNs) was evaluated. The SLN formulation was optimized as: lecithin 100 mg, glycerin monostearate 200 mg, and Tween (1%, w/w). The particle size is around 102 ± 5.2 nm with a PDI of 0.262. The ZP is 30.21 ± 2.05 mV. The prepared SLNs showed high entrapment efficiency of 87.5% for piroxicam. There is no interaction between piroxicam and the vehicle components. The presence of polymorphic form of lipid with higher drug content in the optimized Pir-SLNs enables the Pir-SLNs to release the drug with a sustained manner. Pir-SLNs with oleic acid as enhancer can radically diffuse into both the stratum corneum and dermal layer, as well as penetrate through the hair follicles and sebaceous glands with significantly higher density than the other control groups. Pir-SLNs promptly inhibited the inflammation since the 3rd hour after the treatment by decreasing the PGE2level. SLN was demonstrated to be a promising carrier for encapsulation and sustained release of piroxicam. Pir-SLN is a novel topical preparation with great potential for anti-inflammation application.
authors: a Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University , Hangzhou , P.R. China.
authors: Li-Hua
authors: LH
authors: Peng
authors: a Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University , Hangzhou , P.R. China.|b School of Pharmaceutical Sciences , Jiamushi University , Jiamushi , P.R. China.
authors: Wei
authors: W
authors: Wei
authors: a Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University , Hangzhou , P.R. China.
authors: Ying-Hui
authors: YH
authors: Shan
authors: a Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University , Hangzhou , P.R. China.
authors: Yee-Song
authors: YS
authors: Chong
authors: b School of Pharmaceutical Sciences , Jiamushi University , Jiamushi , P.R. China.
authors: Lian
authors: L
authors: Yu
authors: a Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University , Hangzhou , P.R. China.|c Technology Center for Transdermal Drug Delivery System of Jiangsu Province , Jiangsu , P.R. China.
authors: Jian-Qing
authors: JQ
authors: Gao
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000008:administration & dosage / Q000493:pharmacokinetics*; D065546:Drug Liberation; D004487:Edema / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D053758:Nanoparticles / Q000008:administration & dosage / Q000378:metabolism*; D009924:Organ Culture Techniques; D010894:Piroxicam / Q000008:administration & dosage / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012869:Skin Absorption / Q000187:drug effects* / Q000502:physiology
chemical_list: D000893:Anti-Inflammatory Agents; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D010894:Piroxicam
keywords: Solid lipid nanoparticles; anti-inflammation; piroxicam; topical drug delivery system