Preparation and Evaluation of Pluronic Lecithin Organogel Containing Ricinoleic acid for Transdermal Drug Delivery.

详细信息   

• 作者：Bonam ; Sindhu Prabha.
• 学历：Master
• 年：2013
• 毕业院校：The University of Toledo
• Department：Pharmaceutical Science.
• ISBN：9781303754746
• CBH：1553103
• Country：USA
• 语种：English
• FileSize：1998412
• Pages：118

文摘

Pluronic Lecithin Organogels (PLO gels) are commonly used as transdermal vehicles in compounding pharmacies to provide customized medication for pain management as well as for other therapies. The present research aims at studying the plausibility of using ricinoleic acid as an alternative to isopropyl palmitate in compounding stable PLO gels for pain and inflammation management. In the first part of the study,PLO gel containing ricinoleic acid was prepared and characterized for the transdermal delivery of ketoprofen (10%) and dexamethasone (0.5%). Blank PLO gels were prepared using ricinoleic acid as the oil phase and characterized for pH,viscosity,gelation temperature,and microscopic structure. In-vitro anti-inflammatory activity and cell viability tests were also performed using blank ricinoleic acid PLO and compared with the isopropyl palmitate PLO gel. The optimized PLO gel formulation was further evaluated using ketoprofen (10%) and dexamethasone (0.5%) as model drugs. The stability and in vitro permeability of ketoprofen and dexamethasone was evaluated and compared with the corresponding control formulation (isopropyl palmitate PLO gel). The pH and viscosity of blank PLO gel prepared with ricinoleic acid was comparable with the isopropyl palmitate PLO gel. The anti-inflammatory effect exhibited by the blank ricinoleic acid PLO gel was significantly (p＜0.05) higher than isopropyl palmitate PLO gel at 1 mM concentration,while both the gel formulations had no significant (p＞0.05) cytotoxic activity. Drug loaded PLO gels behaved in a similar manner and all formulations were found to be stable at 25°；C,35°；C,and 40°；C for up to 35 days. The penetration profile of dexamethasone was similar from both the PLO gels,while the permeability for ketoprofen from ricinoleic acid PLO gel was found to be three times higher as compared to the control formulation. The second part of the study deals with the preparation and evaluation of ricinoleic acid PLO gel acid for the transdermal eyelid delivery of tobramycin (0.3%) and dexamethasone (0.1%). PLO gel was characterized for viscosity,pH,gelation temperature,morphology,DSC and drug content. The ex vivo permeability of dexamethasone and bactericidal activity of tobramycin was tested and compared with the marketed TobradexRTM eye ointment. The pH of the optimized ricinoleic acid PLO gel was found to be 6.54 with a gelation temperature of 31°；C. The penetration of dexamethasone from the ricinoleic acid PLO gel was found to be much higher than the marketed TobradexRTM eye ointment. Ricinoleic acid PLO gel containing tobramycin showed a better anti-microbial activity and higher zones of inhibition when compared with the marketed Tobradex RTM eye ointment. The findings of this investigation indicate that the ricinoleic acid PLO gel has the potential for use as a transdermal eyelid delivery system. Ricinoleic acid PLO gel was found to be better than the commercial TobradexRTM eye ointment with respect to the penetration of dexamethasone and anti-microbial activity of tobramycin.