The role of surfactants in the formulation of elastic liposomal gels containing a synthetic opioid analgesic.
Transdermal drug delivery systems have made significant contributions to the medical community, but have yet to completely substitute oral or parenteral delivery. Recently, various strategies have been used to augment the transdermal delivery of therapeutics. Primarily, they include iontophoresis, electrophoresis, sonophoresis, chemical permeation enhancers, microneedles, and vesicular systems. Among these strategies, elastic liposomes appear promising. Elastic vesicle scaffolds have been developed and evaluated as novel topical and transdermal delivery systems, with an infrastructure consisting of hydrophobic and hydrophilic moieties together, and as a result, such scaffolds can accommodate drug molecules with a wide range of solubility. High deformability of these vesicles provides for better penetration of intact vesicles. This system is much more efficient at delivering low- and high-molecular-weight drugs to the skin in terms of quantity and depth. In this work, elastic liposomes of Tramadol HCl were prepared using a solvent evaporation method with different surfactants and were characterized using microscopy, and particle size, shape, drug content, ex vivo release, and zeta potential were also calculated. The prepared elastic liposomes were found to be in the range of 152.4 nm with a zeta potential of -22.4 mV; the entrapment efficiencies of the selected formulation was found to be 79.71%±0.27%. All formulations in the form of a gel were evaluated for physicochemical properties and were found to be homogeneous with no grittiness, and the pH of all formulations was found to be neutral. The optimized selected elastic liposomal formulation followed the Higuchi equation and Fickian diffusion and released the drug for a period of 24 hours. The overall results provide much promise for the continued investigation of deformable vesicles as transdermal drug carriers.
School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, India.
Sima
S
Singh
School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, India.
Harsh
H
Vardhan
Center for Research in Medical Devices, National University of Ireland, Galway, Ireland.
Niranjan G
NG
Kotla
Department of Pharmaceutics, Vishwabharathi College of Pharmaceutical Sciences, Guntur, India.
Balaji
B
Maddiboyina
Ranbaxy Laboratory Ltd, Gurgaon, India.
Dinesh
D
Sharma
Department of Chemical Engineering, Northeastern University, Boston, MA, USA; Center of Excellence for Advanced Materials Research, King Abdulaziz University, Jeddah, Saudi Arabia.
Thomas J
TJ
Webster
D000279:Administration, Cutaneous; D000701:Analgesics, Opioid / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers / Q000378:metabolism; D004339:Drug Compounding; D004548:Elasticity; D005079:Excipients; D005782:Gels / Q000008:administration & dosage* / Q000737:chemistry; D057927:Hydrophobic and Hydrophilic Interactions; D008081:Liposomes / Q000737:chemistry*; D010316:Particle Size; D051381:Rats; D012867:Skin / Q000187:drug effects*; D012869:Skin Absorption; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry*
D000701:Analgesics, Opioid; D004337:Drug Carriers; D005079:Excipients; D005782:Gels; D008081:Liposomes; D013501:Surface-Active Agents
elastic liposome; hydration-gradient; hydrogel; occlusion; skin delivery