An Injectable Gel Platform for the Prolonged Therapeutic Effect of Pitavastatin in the Management of Hyperlipidemia

In this study, an injectable in situ forming gel has been designed and fabricated for the controlled and prolonged release of pitavastatin calcium (Pit) for treating hyperlipidemia. By mixing phospholipids and soybean oil with ethanol, the phospholipid-based platform material (PSE) displayed in a sol state with low viscosity in vitro. After subcutaneous injection, pregel solution underwent rapid-phase separation and gelation in situ thus forming a drug release depot. Pit was loaded within PSE (PSE-P), which achieved prolonged release profiles for 15 consecutive days in vitro. Correspondingly, the pharmacokinetic study in rats demonstrated that PSE-P achieved sustained in vivo release for 15 days after 1 subcutaneous injection. The pharmacodynamic study in hyperlipidemia rats further revealed that the levels of total cholesterol, total triglyceride, and low-density lipoprotein decreased remarkably, and the in vivo therapeutic effect was well maintained for over 20 days. Additionally, PSE-P showed mild tissue inflammatory responses and excellent degradability in vivo. Thus, in situ forming PSE-P gel represents a viable and promising drug delivery platform to achieve long-term therapeutic effects in the management of hyperlipidemia. (C) 2016 American Pharmacists Association. Published by Elsevier Inc. All rights reserved.