Double-liposome-based dual-drug delivery system as vectors for effective management of peptic ulcer.
The aim of the present investigation was to prepare and evaluate a vesicular dual-drug delivery system for effective management of the mucosal ulcer. Inner encapsulating and double liposomes were prepared by the glass-bead and reverse-phase evaporation methods, respectively. The formulation consisted of inner liposomes bearing ranitidine bismuth citrate (RBC) and outer liposomes encapsulating amoxicillin trihydrate (AMOX). The optimized inner liposomes and double liposomes were extensively characterized for vesicle size, morphology, zeta potential, vesicles count, entrapment efficiency, and in vitro drug release. In vitro, the double liposomes demonstrated a sustained release of AMOX and RBC of 93.6 ± 1.9 and 84.1 ± 0.9%, respectively, at the end of 144 hours. Ex vivo studies were conducted on Helicobacter pylori (ATCC26695) bacterial cell lines. Double liposomes showed a more enhanced percent H. pylori growth inhibition than the plain drug combination. Further, in vivo studies illustrated enhanced antisecretory and ulcer-protective activity of double liposomes, as compared to the plain drug combination. Microscopic studies also supported the ulcer-protective action of the formulation. Thus, it may be concluded that double liposomes are instrumental in reducing gastric secretions and targeting ulcer sites with the interception of minimal side effects, thus suggesting their potential in ulcer therapy.
Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences, Dr. H.S. Gour University, Sagar, India.
Ashish K
AK
Jain
Abhinav
A
Agarwal
Himanshu
H
Agrawal
Govind P
GP
Agrawal
D000658:Amoxicillin / Q000008:administration & dosage* / Q000737:chemistry; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000494:pharmacology; D000897:Anti-Ulcer Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D001729:Bismuth / Q000008:administration & dosage* / Q000737:chemistry; D003692:Delayed-Action Preparations / Q000008:administration & dosage* / Q000737:chemistry; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry; D004338:Drug Combinations; D004355:Drug Stability; D005260:Female; D005753:Gastric Mucosa / Q000737:chemistry / Q000187:drug effects; D016481:Helicobacter Infections / Q000382:microbiology; D016480:Helicobacter pylori / Q000187:drug effects; D008081:Liposomes; D008297:Male; D008826:Microbial Sensitivity Tests; D010316:Particle Size; D010437:Peptic Ulcer / Q000188:drug therapy* / Q000473:pathology; D011899:Ranitidine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry; D051381:Rats
D000900:Anti-Bacterial Agents; D000897:Anti-Ulcer Agents; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004338:Drug Combinations; D008081:Liposomes; C073340:ranitidine bismuth citrate; D000658:Amoxicillin; D011899:Ranitidine; D001729:Bismuth