Development of curcuminoids loaded poly(butyl) cyanoacrylate nanoparticles: Physicochemical characterization and stability study

• Published in: European journal of pharmaceutical sciences 2009-06, Vol.37 (3), p.395-404
• Main Authors: Mulik, Rohit, Mahadik, Kakasaheb, Paradkar, Anant
• Format: Article
• Language: English
• Subjects: Algorithms; Anti-Inflammatory Agents, Non-Steroidal - administration & dosage; Bioavailability; Biological and medical sciences; Biological Availability; Calorimetry, Differential Scanning; Chromatography, Gel; Controlled release; Curcumin - administration & dosage; Curcumin - analogs & derivatives; Curcuminoids; Cyanoacrylates; Delayed-Action Preparations; Drug Compounding; Drug Stability; General pharmacology; Magnetic Resonance Spectroscopy; Medical sciences; Microscopy, Electron, Transmission; Nanoparticles; Particle Size; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Poloxamer; Poly(butyl) cyanoacrylate; Solubility; Stability; Surface Properties; Surface-Active Agents
• ISSN: 0928-0987; 1879-0720
• DOI: 10.1016/j.ejps.2009.03.009

Curcumininoids, obtained from the rhizomes of Curcuma longa L., Zingiberaceae (turmeric), are the most widely used phytoconstituent in food industry and recently for its therapeutic activity. It has very wide spectrum of therapeutic use like in inflammation, psoriasis, various tumors, wound healing and also in neurodegenerative diseases like Alzheimer's disease. But its highly lipophilic nature and very poor bioavailability hampers its therapeutic usefulness. Poly(butyl) cyanoacrylate (PBCA) nanoparticles coated with poloxamer 188 containing curcuminoids were prepared by anionic polymerization using solvent evaporation method. The particle size and zeta potential of prepared liposomes was 178 nm and −28.33 respectively with 77.99% encapsulation efficiency. The TEM study revealed the spherical nature of the prepared nanoparticles alongwith confirmation of particle size. The polymerization and entrapment of curcuminoids was confirmed using H 1 NMR study by comparing the spectra of nanoparticles with that of curcuminoids. DSC study revealed that curcuminoids was entrapped inside the nanoparticles in molecular dispersion form. In vitro release study showed that the prepared PBCA nanoparticles are capable of controlled drug release (following matrix model) for extended period of time with higher release in acidic environment compared to PB 7.4 suggesting the usefulness of the prepared nanoparticles for intracellular delivery. The mean particle size, zeta potential and the amount of curcuminoids showed no significant changes compared to the freshly prepared PBCA nanoparticles after storage for 6 months at 40 °C/75% RH in the presence and absence of sunlight.