title: Development of grafted xyloglucan micelles for pulmonary delivery of curcumin: In vitro and in vivo studies.
abstract: A novel grafted copolymer consisting of l-lactide grafted xyloglucan was synthesized by polymerization reaction and characterized. The grafted copolymers were analyzed by Fourier-transform infrared spectrometry (FTIR) and (1)H nuclear magnetic resonance ((1)H NMR) was performed to confirm the grafting of l-poly lactic acid on xyloglucan. The grafted polymer forms micelles at the critical micelle concentration of 0.0150 wt% with the average particle size of 102 nm, as determined by particle size analyzer. The zeta potential of the curcumin loaded micelles was -18.2 mV, an acceptable drug loading efficiency of 68.9 ± 0.02% and the entrapment efficiency of 96.38 ± 0.2%. The release study for 5h showed a sustained release property. In vitro assessment demonstrates suitability of micelles as dry powder for inhalation. In vivo studies showed significant improvement in bioavailability on pulmonary administration of curcumin micelles as DPI formulation. The potential for pulmonary delivery curcumin loaded in micelles was evaluated. In conclusion, polymeric micelle based on a newly synthesized grafted xyloglucan could be suitable carrier for pulmonary delivery of curcumin.
authors.affiliation: R.C. Patel Institute of Pharmaceutical Education and Research, Shirpur, Dhule, India. Electronic address: hsmahajan@rediffmail.com.
authors.forename: Hitendra S
authors.initials: HS
authors.lastname: Mahajan
authors.affiliation: R.C. Patel Institute of Pharmaceutical Education and Research, Shirpur, Dhule, India.
authors.forename: Prashant R
authors.initials: PR
authors.lastname: Mahajan
mesh_terms: D000818:Animals; D002626:Chemistry, Pharmaceutical; D003474:Curcumin / Q000008:administration & dosage* / Q000737:chemistry* / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000737:chemistry; D065546:Drug Liberation; D058995:Dry Powder Inhalers; D005936:Glucans / Q000737:chemistry*; D008168:Lung / Q000187:drug effects / Q000378:metabolism; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D008823:Micelles; D010316:Particle Size; D011108:Polymers / Q000138:chemical synthesis / Q000737:chemistry; D051381:Rats; D017550:Spectroscopy, Fourier Transform Infrared; D014990:Xylans / Q000737:chemistry*
chemical_list: D004337:Drug Carriers; D005936:Glucans; D008823:Micelles; D011108:Polymers; D014990:Xylans; C029353:xyloglucan; D003474:Curcumin
keywords: Curcumin; Drug release; Grafted polymer; Micelles; Xyloglucan