title: A study on ethosomes as mode for transdermal delivery of an antidiabetic drug.
abstract: BACKGROUND
  A transdermal delivery system is warranted for repaglinide (RPG) which possesses half-life of 1 h and oral bioavailability of 56%. Ethosomes are useful tools for transdermal drug delivery.
  
  
  OBJECTIVE
  To prepare and evaluate ethosomes as mode for transdermal delivery of RPG.
  
  
  METHODS
  Ethosomes loaded with RPG were prepared from dipalmitoyl phosphatidylcholine and ethanol by the cold method. They were characterized using Fourier transform infrared spectroscopy and differential scanning calorimetry. They were evaluated for vesicle size, entrapment efficiency and ex-vivo skin permeation. Ethosomal composition was optimized using the 3(2) factorial design. Gel containing optimzsed ethosomes was studied for antidiabetic activity in rats.
  
  
  RESULTS
  RPG ethosomes possessing the size of 0.171-1.727 µm and entrapment efficiency of 75-92% were obtained. They demonstrated a significantly higher permeation (64-97% of the administered dose) across excised rat skin when compared to free drug and its hydro alcoholic solution. In-vivo, RPG ethosomal system caused sustained antidiabetic effect.
  
  
  CONCLUSIONS
  The lipid and ethanol concentration affected the physicochemical attributes and performance of ethosomes. The flexible ethosomes permeated the stratum corneum and improvized the availability of RPG for antidiabetic action. They prolonged the antidiabetic effect of RPG over a significantly longer period of time in comparison with the equivalent oral dose.
  
  
  CONCLUSIONS
  Ethosomal system can successfully deliver RPG transdermally; sustain its effect and thus reduce its dosing frequency. Ethosomes are useful for enhancing the efficacy of RPG in the treatment of diabetes.
authors: Department of Pharmaceutics, Modern College of Pharmacy, Pune, Maharashtra, India.
authors: Siddhodhan S
authors: SS
authors: Bodade
authors: Karimunnisa Sameer
authors: KS
authors: Shaikh
authors: Meghana S
authors: MS
authors: Kamble
authors: Praveen D
authors: PD
authors: Chaudhari
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D002219:Carbamates / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism; D016503:Drug Delivery Systems / Q000379:methods*; D007004:Hypoglycemic Agents / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism; D009924:Organ Culture Techniques; D010880:Piperidines / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D012869:Skin Absorption / Q000187:drug effects / Q000502:physiology
chemical_list: D002219:Carbamates; D004337:Drug Carriers; D007004:Hypoglycemic Agents; D010880:Piperidines; C072379:repaglinide