Ethosomes could enhance cell membrane fluidity and reduce epidermal membrane density to make macromolecular drugs through the stratum corneum into the deeper layers of the skin easily. Methods: We used the orthogonal method to optimize the formulation of the ethosome preparation prepared by the ethonal infusion method. Ethosomal gels were characterized by using different analytical methods. Transdermal release rate in vitro have been demonstrated in Franz diffusion cells and the efficacy of drug-loaded nanocarriers in vivo was investigated in a mouse model.
|Published (Last):||16 July 2019|
|PDF File Size:||12.81 Mb|
|ePub File Size:||20.9 Mb|
|Price:||Free* [*Free Regsitration Required]|
University of Baroda, Shri G. Thakkar, Email: moc. Corresponding author. Received Jul 12; Accepted Oct 3. Abstract The aim was to develop niosomal gel as a transdermal nanocarrier for improved systemic availability of lopinavir. Niosomes were prepared using thin-film hydration method and optimized for molar quantities of Span 40 and cholesterol to impart desirable characteristics.
Comparative evaluation with ethosomes was performed using ex vivo skin permeation, fluorescence microscopy, and histopathology studies. Clinical utility via transdermal route was acknowledged using in vivo bioavailability study in male Wistar rats.
The niosomal formulation containing lopinavir, Span 40, and cholesterol in a molar ratio of Ex vivo skin permeation studies of lopinavir as well as fluorescent probe coumarin revealed a better deposition of ethosomal carriers but a better release with niosomal carriers. Histopathological studies indicated the better safety profile of niosomes over ethosomes.
Taken together, these findings suggested that niosomal gel holds a great potential of being utilized as novel, nanosized drug delivery vehicle for transdermal lopinavir delivery. Interventions such as AIDS counseling, educational tools, and antiretroviral drug therapy have contributed to transforming HIV infection from a fatal to a manageable chronic infectious disease.
However, as per the global report by UNAIDS in 2 , the number of people receiving therapy has grown fold since , including more than five million people in low- and middle-income countries. Hence, despite available preventive measures, much remains to be accomplished as the number of newly reported HIV infections still remains unacceptably high. Lopinavir, 2S -N-[ 2S,4S,5S [2- 2,6-dimethylphenoxy -acetamido]hydroxy-1,6-diphenylhexanyl]methyl 2-oxo-1,3-diazinanyl -butanamide, a specific reversible inhibitors of the HIV protease, exerts its effect against HIV infection by blocking the ability of the protease to cleave the Gag-Pol polyprotein, resulting in the production of immature, noninfectious viral particles.
Though the marketed tablet and capsule formulations of lopinavir are generally combined with Ritonavir, a potent inhibitor of cytochrome P 3A4, to minimize presystemic metabolism of lopinavir 4 , other challenges contributing to poor oral absorption remain unanswered. Hence, to overcome all the limitations associated with oral administration of lopinavir and to promote single drug administration, utilization of vesicular nanocarriers through transdermal route could prove to be effective, as the approach combines the inherent advantages of transdermal route and the drug carrying potential of vesicular nanocarriers across the tough and otherwise impervious skin barrier layer, i.
Among several nanovesicular carriers, niosome is selected here as a carrier of choice owing to its dominance over conventional liposomes with respect to stability and cost-effectiveness. Niosome contains several concentric bilayer membrane mainly composed of nonionic surfactants and cholesterol enclosing aqueous phase in the core.
Niosomes are known to improve the solubility, bioavailability, and stability of some poorly soluble drugs 5 — 8 along with an ability to provide sustained release for prolonged drug action 9. Surfactants contribute to the overall penetration enhancement of compounds primarily by adsorption at interfaces, by interacting with biological membranes and by alteration of the barrier function of the SC, as a result of reversible lipid modification Ethosomes, soft, malleable lipid vesicles with high ethanol content tailored for enhanced transdermal delivery of active agents 11 , are used for comparative study wherever required.
So, the aim of the present work was to develop lopinavir-loaded niosomal gel and characterize it for its usefulness as a transdermal nanocarrier in delivering therapeutically sufficient quantity of lopinavir to combat against AIDS. Span 40, cholesterol, carbopol, coumarin, chloroform, and methanol were purchased from S. Fine Chemicals, India. Nuclepore polycarbonate membrane 0.
Water distilled prepared in laboratory by distillation. All the chemicals and reagents used were of analytical grade. The solvent was evaporated in the rotary flash evaporator until thin, dry, and uniform film is formed. Niosomal dispersion supernatant was then decanted and characterized for vesicle size and percentage of drug entrapment PDE while the drug pellet sediment was used to measure unentrapped drug in order to ascertain mass balance.
The formulation process parameters were optimized to achieve maximum possible drug entrapment with desirable size range
Nanoethosomal gel from ashitaba leaves for burn treatment
Burn wounds are caused by direct contact with heat or radiation, radioactivity, electricity, friction or chemicals with a 0. According to the World Health Organization , there are , deaths every year worldwide due to burn wounds. In Indonesia, burn wounds cause , people die every year. Under the guidance of Dr. Lilik Maslachah. Afif also said that Ashitaba was chosen because it has great potential as traditional medicine.
Novel ethosomal gel of clove oil for the treatment of cutaneous candidiasis.
Objective: The aim of the current investigation is to formulate and optimize a topical BDH ethosomal gel for weight gain control. The morphology and zeta potential of the optimized formulation were evaluated. Results: The size and entrapment efficiency percent had a direct positive relationship with the concentration of PC and negative relationship with ethanol and PG. Regression modeling indicated a good correlation between dependent and independent variables, where F16 was chosen as the optimized formulation. Food intake and weight gain of rats were significantly decreased after transdermal application of the BDH ethosomal gel when compared with control, placebo, and BDH gel.