title: Embelin lipid nanospheres for enhanced treatment of ulcerative colitis - Preparation, characterization and in vivo evaluation.
abstract: Aim of the present study is to develop embelin lipid nanospheres (LNE) for better treatment of ulcerative colitis. Embelin LNs were developed using soya bean oil/virgin coconut oil as liquid lipid carrier and soya/egg lecithin as stabilizer by hot homogenization followed by ultrasonication technique. The particle size of LNEs ranged from 196.1±3.57 to 269.2±1.05nm with narrow polydispersity index values whereas zeta potential was from -36.6 to -62.0mV. Embelin was successfully incorporated into lipid nanospheres with entrapment efficiency about 99%. There was no interaction between embelin and selected liquid lipids which was confirmed by FTIR studies. In vitro drug release studies performed using Franz diffusion cell and results showed sustained release of embelin. Embelin LNs were stabilized with egg and soya lecithin, embelin release from these LNs followed Higuchi model and first order model, respectively, however mechanism of drug release in both LNs was non-Fickian. In vivo studies were carried out using acetic acid induced ulcerative colitis rat model and results revealed that treatment with embelin LNs significantly reduced clinical activity and macroscopic scores compared to embelin conventional suspension. Treatment with embelin LNs decreased MPO, LDH and LPO levels, increased reduced GSH levels which indicated better treatment of ulcerative colitis was achieved. This was also confirmed by improved histopathological conditions. Thus embelin LNs could be favourably used for treatment of ulcerative colitis.
authors.affiliation: Sree Siddaganga College of Pharmacy, Tumkur, Karnataka, India.
authors.forename: Shivaram Shivakumar
authors.initials: SS
authors.lastname: Badamaranahalli
authors.affiliation: Sree Siddaganga College of Pharmacy, Tumkur, Karnataka, India. Electronic address: manju_kop@yahoo.com.
authors.forename: Manjunath
authors.initials: M
authors.lastname: Kopparam
authors.affiliation: Sree Siddaganga College of Pharmacy, Tumkur, Karnataka, India; Manipal College of Pharmaceutical Sciences, Manipal, Karnataka, India.
authors.forename: Siddalingappa Tippanna
authors.initials: ST
authors.lastname: Bhagawati
authors.affiliation: Sree Siddaganga College of Pharmacy, Tumkur, Karnataka, India.
authors.forename: Sharanbasappa
authors.initials: S
authors.lastname: Durg
mesh_terms: D019342:Acetic Acid; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D016227:Benzoquinones / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D002626:Chemistry, Pharmaceutical; D000074263:Coconut Oil; D003093:Colitis, Ulcerative / Q000139:chemically induced / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D003106:Colon / Q000187:drug effects / Q000378:metabolism / Q000473:pathology; D003692:Delayed-Action Preparations; D004058:Diffusion; D004195:Disease Models, Animal; D005079:Excipients; D005765:Gastrointestinal Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D007700:Kinetics; D007770:L-Lactate Dehydrogenase / Q000378:metabolism; D054709:Lecithins / Q000737:chemistry; D015227:Lipid Peroxidation / Q000187:drug effects; D008297:Male; D008956:Models, Chemical; D054118:Nanospheres; D009195:Peroxidase / Q000378:metabolism; D010938:Plant Oils / Q000737:chemistry*; D017208:Rats, Wistar; D012995:Solubility; D013010:Sonication; D013024:Soybean Oil / Q000737:chemistry*; D017550:Spectroscopy, Fourier Transform Infrared; D013678:Technology, Pharmaceutical / Q000379:methods; D014465:Ultrasonics
chemical_list: D000893:Anti-Inflammatory Agents; D016227:Benzoquinones; D003692:Delayed-Action Preparations; D005079:Excipients; D005765:Gastrointestinal Agents; D054709:Lecithins; D010938:Plant Oils; D013024:Soybean Oil; D007770:L-Lactate Dehydrogenase; D009195:Peroxidase; D019342:Acetic Acid; D000074263:Coconut Oil; C010945:embelin
keywords: Embelin; FTIR; Lipid nanospheres; Soya bean oil; Ulcerative colitis; Virgin coconut oil