title: Enteric-coated alendronate sodium nanoliposomes: a novel formula to overcome barriers for the treatment of osteoporosis.
abstract: OBJECTIVE
  Alendronate sodium (ALS) is the most common drug used for the treatment of osteoporosis. The challenges facing ALS use include: very poor oral bioavailability (0.6%), esophageal ulcers, and complicated instructions for its use. The objective of this research is to utilize nanotechnology to formulate ALS into enteric-coated nanoliposomes (NLS) to overcome the previously mentioned drawbacks.
  
  
  METHODS
  NLS were prepared with lipid components of phosphatidylcholine (PC), cholesterol (CH), and lecithin (Lec) in ratios 4:1:1, 4:2:1, 4:3:1, and 4:4:1, respectively. Formulas that showed the highest entrapment efficiency were prepared either alone or mixed with positive and negative charge-inducing agents and coated with Eudragit L100. Eudragit-coated NLS (EuC-NLS) were evaluated for particle size, zeta potential, morphological examination, and drug release in pH 1.2 and pH 7.4 media. The pharmacokinetic study was carried out in rabbits.
  
  
  RESULTS
  Spherical NLS were successfully developed with a mean size range from 70 to 150 nm. EuC-NLS with PC:CH:Lec:dicetyl phosphate (4:3:1:1) successfully resist the release of ALS in acidic environments and enhanced the bioavailability in rabbits 12-fold compared with the marketed tablets.
  
  
  CONCLUSIONS
  EuC-NLS is a promising novel formula for ALS with higher bioavailability and a lower dose, avoiding the side effects of esophageal ulceration.
authors: King Abdulaziz University, Faculty of Pharmacy, Department of Pharmaceutics, Jeddah, Saudi Arabia. Elswaify2000@yahoo.com
authors: Khaled Mohamed
authors: KM
authors: Hosny
authors: Osama Abdelhakim Aly
authors: OA
authors: Ahmed
authors: Rana Tariq
authors: RT
authors: Al-Abdali
mesh_terms: D019386:Alendronate / Q000737:chemistry / Q000493:pharmacokinetics*; D000818:Animals; D001682:Biological Availability; D050071:Bone Density Conservation Agents / Q000737:chemistry / Q000493:pharmacokinetics*; D002626:Chemistry, Pharmaceutical; D020099:Coated Materials, Biocompatible / Q000737:chemistry*; D016503:Drug Delivery Systems; D006863:Hydrogen-Ion Concentration; D007408:Intestinal Absorption; D007413:Intestinal Mucosa / Q000378:metabolism; D008081:Liposomes; D008297:Male; D010024:Osteoporosis / Q000188:drug therapy*; D010316:Particle Size; D011109:Polymethacrylic Acids / Q000737:chemistry*; D011817:Rabbits
chemical_list: D050071:Bone Density Conservation Agents; D020099:Coated Materials, Biocompatible; D008081:Liposomes; D011109:Polymethacrylic Acids; C038300:methylmethacrylate-methacrylic acid copolymer; D019386:Alendronate