Anti-Inflammatory Effects of Novel Standardized Solid Lipid Curcumin Formulations

Abstract

Inflammation and the presence of pro-inflammatory cytokines are associated with numerous chronic diseases such as type-2 diabetes mellitus, cardiovascular disease, Alzheimer's disease, and cancer. An overwhelming amount of data indicates that curcumin, a polyphenol obtained from the Indian spice turmeric, Curcuma longa, is a potential chemopreventive agent for treating certain cancers and other chronic inflammatory diseases. However, the low bioavailability of curcumin, partly due to its low solubility and stability in the digestive tract, limits its therapeutic applications. Recent studies have demonstrated increased bioavailability and health-promoting effects of a novel solid lipid particle formulation of curcumin (Curcumin SLCP, Longvida Ò ). The goal of this study was to evaluate the aqueous solubility and in vitro anti-inflammatory effects of solid lipid curcumin particle (SLCP) formulations using lipopolysaccharide (LPS)-stimulated RAW 264.7 cultured murine macrophages. SLCPs treatment significantly decreased nitric oxide (NO) and prostaglandin-E2 (PGE2) levels at concentrations ranging from 10 to 50 lg/mL, and reduced interleukin-6 (IL-6) levels in a concentration-dependent manner. Transient transfection experiments using a nuclear factor-kappa B (NF-jB) reporter construct indicate that SLCPs significantly inhibit the transcriptional activity of NF-jB in macrophages. Taken together, these results show that in RAW 264.7 murine macrophages, SLCPs have improved solubility over unformulated curcumin, and significantly decrease the LPSinduced pro-inflammatory mediators NO, PGE2, and IL-6 by inhibiting the activation of NF-jB. KEY WORDS: curcumin inflammation interleukin-6 interleukin-1b LongvidaÒ NF-jB nitric oxide prostaglandin-E2

Effects of Micro-environmental pH of Liposome on Chemical Stability of Loaded Drug

“…It is well known that curcumin is a lipophilic molecule and has been extensively used in food, medicines, and cosmetics due to its various bioactivities [17][18][19][20][21]. However, its delivery is highly limited by its insolubility and instability in biological fluids [22][23][24][25]. So far, it is yet to fulfill its clinical promise in part due to pH-mediated instability [26].…”

Preservation of dendritic spine morphology and postsynaptic signaling markers after treatment with solid lipid curcumin particles in the 5xFAD mouse model of Alzheimer’s disease

“…Within the lipid core, the curcumin was coated. The SLCP formulation has been characterized by our laboratory and others with in vitro [30], and in animal models [23,[31][32][33], as well as in clinical trials of AD [34]. Detailed information for all the antibodies used in this study are documented in Table 5.…”

Phytobioactive compound-based nanodelivery systems for the treatment of type 2 diabetes mellitus – current status

“…[128][129][130][131] However, it has low potential through oral delivery due to the low water solubility and stability in gastrointestinal environment. [132][133][134][135][136] Nanodelivery systems are an alternative approach that can improve the stability of those compounds with improved bioavailability of curcumin. [137][138][139][140][141][142][143][144][145][146][147][148][149][150] Curcumin-loaded PLGA NPs were constructed with a particle size of 281 nm, and these have shown a higher bioavailability through oral delivery in the diabetic rat model, delaying cataracts.…”