title: Comparison of pharmaceutical nanoformulations for curcumin: Enhancement of aqueous solubility and carrier retention.
abstract: Curcumin, originally used in traditional medicine and as a spice, is one of the most studied and most popular natural products of the past decade. It has been described to be an effective anti-inflammatory and anti-cancer drug and protects against chronic diseases such as rheumatoid arthritis and atherosclerosis. Despite these promising pharmacological properties, curcumin is also very lipophilic, which makes its formulation challenging. Ideally the nanocarrier should additionally also retain the encapsulated curcumin to provide target tissue accumulation. In this study we aimed to tackle this aqueous solubility and carrier retention challenge of curcumin by encapsulating curcumin in different nanoparticles. We successfully loaded LDL (30nm), polymeric micelles (80nm), liposomes (180nm) and Intralipid (280nm) with curcumin. The relative loading capacity was inversely related to the size of the particle. The stability for all formulations was determined in fetal bovine serum over a course of 24h. Although all curcumin-nanoparticles were stable in buffer solution, all leaked more than 70% of curcumin under physiological conditions. Altogether, tested nanoparticles do solve the aqueous insolubility problem of curcumin, however, because of their leaky nature, the challenge of carrier retention remains.
authors.affiliation: Department of Biomaterials Science and Technology, University of Twente, Enschede, The Netherlands. Electronic address: i.e.allijn@utwente.nl.
authors.forename: Iris E
authors.initials: IE
authors.lastname: Allijn
authors.affiliation: Clinical Chemistry and Haematology, University Medical Centre, Utrecht, The Netherlands.
authors.forename: Raymond M
authors.initials: RM
authors.lastname: Schiffelers
authors.affiliation: Department of Biomaterials Science and Technology, University of Twente, Enschede, The Netherlands; Department of Pharmaceutics, Utrecht University, Utrecht, The Netherlands.
authors.forename: Gert
authors.initials: G
authors.lastname: Storm
mesh_terms: D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003474:Curcumin / Q000008:administration & dosage* / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry*; D004355:Drug Stability; D004655:Emulsions / Q000737:chemistry; D008077:Lipoproteins, LDL / Q000737:chemistry; D008081:Liposomes; D008823:Micelles; D053758:Nanoparticles; D010316:Particle Size; D010743:Phospholipids / Q000737:chemistry; D011108:Polymers / Q000737:chemistry; D012995:Solubility; D013024:Soybean Oil / Q000737:chemistry
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D004655:Emulsions; D008077:Lipoproteins, LDL; D008081:Liposomes; D008823:Micelles; D010743:Phospholipids; D011108:Polymers; C545823:soybean oil, phospholipid emulsion; D013024:Soybean Oil; D003474:Curcumin
keywords: Curcumin; Curcumin (Pubchem CID:969516); Drug delivery; Lipophilic drugs; Nanoparticles