Formulation and in vitro Evaluation of Topical Liposomal Gel of Triamcinolone Acetonide (original) (raw)
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International Journal of Health Sciences (IJHS), 2022
Background and objective: Applying liposomal gels in transdermal drug delivery system has evoked considerable interest because of their good activity for osteoarthritis. The aim of present study was to prepare and characterize liposomes of NSAIDS drug meloxicam, which may deliver these drugs to the target site more efficiently and also overcome the problem related with oral drug delivery of the drug. Methodology: In the present investigation efficiency of liposomes as a novel lipid for topical delivery of meloxicam has been evaluated. Liposomes were optimize by varying concentration of phospholipids cholesterol and ethanol. Liposomes formulation with soya lecithin, cholesterol and ethanol was optimized. Result: On characterization spherical, unilamellar vesicle with smooth surface were observed under Scanning electron microscopy and F4 formulation shows the best result. Conclusion: Suggested as liposomes as an efficient carriers for meloxicam topical drug delivery.
TOPICAL LIPOSOMAL GEL: A NEW STRATEGY OF NOVEL DRUG DELIVERY
Liposomes established themselves as a promising novel drug delivery vehicle in several different basic sciences and as a viable alternative in several applications. Liposomes are microscopic spheres with an aqueous core surrounded by one or more outer shells consisting of lipids arranged in a bilayer configuration. Liposomes are acceptable and superior carriers having ability to encapsulate hydrophilic and lipophilic drugs and protect them from degradation. It also has affinity to keratin of horny layer of skin and can penetrate deeper into skin and hence give better absorption. Applied on the skin, liposomes may act as a solublizing matrix for poorly soluble drugs, penetration enhancer as well as local depot at the same time diminishing the side effects of these drugs. Topical liposome formulations could be more effective and less toxic than conventional formulations. The liposome gel formulations could perform therapeutically better effects than the conventional formulations, as prolonged and controlled release topical dosage forms, which may lead to improved efficiency and better patient compliance.
Artificial Cells, Nanomedicine, and Biotechnology, 2016
Triamcinolone acetonide (TA) employed for the treatment of atopic dermatitis exhibits limited penetration into the epidermis. This investigation aimed to explore the role of binary solvents in topical drug delivery of TA by developing nanoethosomal glycolic lipid vesicles by infusion method. Screening of vesicles (TA1-TA17) formulated by Box Behnken design identified the optimized formulation (TA10) that was developed as carbomer gels. The gels were then evaluated for pharmaceutical properties and compared with control and reference ethosomal gel (RG). Higher in vitro permeation was found in gels containing TA10, prepared with or without using penetration enhancer (EGP 83.76 ± 0.72% and EG 82.42 ± 0.89%, respectively). CLSM studies depicted deeper uniform penetration of fluorescent tracer into the epidermis via EG as compared with RG and control gel. Enhanced penetration was due to combinational solvent effect exerted by ethanol and propylene glycol. Histological analysis confirmed the nonirritant potential of the gel. Thus, it can be concluded that nanoethosomal glycolic vesicles proved to be an effective non irritant carrier for improvised penetration of triamcinolone acetonide for potential topical therapeutics.
Artificial cells, nanomedicine, and biotechnology, 2016
Triamcinolone acetonide (TA) employed for the treatment of atopic dermatitis exhibits limited penetration into the epidermis. This investigation aimed to explore the role of binary solvents in topical drug delivery of TA by developing nanoethosomal glycolic lipid vesicles by infusion method. Screening of vesicles (TA1-TA17) formulated by Box Behnken design identified the optimized formulation (TA10) that was developed as carbomer gels. The gels were then evaluated for pharmaceutical properties and compared with control and reference ethosomal gel (RG). Higher in vitro permeation was found in gels containing TA10, prepared with or without using penetration enhancer (EGP 83.76 ± 0.72% and EG 82.42 ± 0.89%, respectively). CLSM studies depicted deeper uniform penetration of fluorescent tracer into the epidermis via EG as compared with RG and control gel. Enhanced penetration was due to combinational solvent effect exerted by ethanol and propylene glycol. Histological analysis confirmed ...
2021
Psoriasis is an autoimmune disorder characterized by hyper proliferation of the epidermal layer at the typical body sites, including nails, scalps, cleft and knees. Liposomes are the best carrier for effective delivery of bioactives in the deep skin areas. In the present study, a comparative study of liposomes was carried out using thin film hydration and curvature tuned methods. Liposomes were prepared using cholesterol, soy lecithin and Span 80. The liposomes were evaluated for physical characterization, morphology, surface charge and release properties. Liposomes prepared by the thin film hydration method (formulation TACTL2) had better properties compared to liposomes prepared by the curvature tuned method (formulation TACCT2) in terms of entrapment efficiency (78.5±1.8% vs 53.4±5.6%), particle size (411.8 nm vs 630 nm), surface morphology(round and dispersed particles vs aggregates and lumps), and release profile (70.1% vs 32.87% in 12 h). Based on the results it is concluded that the thin film hydration method is better than a curvature tuned method for the preparation of liposomes.
Development of novel topical tranexamic acid liposome formulations
International journal of pharmaceutics, 2002
The aims of this study were to develop novel liposome formulations for tranexamic acid (TA) from various lipid compositions [neutral (hydrogenated soya phosphatidylcholine and cholesterol), positive (stearylamine) or negative (dicetyl phosphate) charged lipid], and to investigate the effects of concentrations of TA (5 and 10% in DI water) and charges on the physicochemical properties of liposomes. Liposomes were prepared by chloroform film method with sonication. The physical (appearance, pH, size, morphology) and chemical (drug encapsulation efficiency, transition temperature, enthalpy of transition) properties of liposomes were characterized. The TA contents were determined spectrophotometrically at 415 nm, following derivatization with 2,4,6-trinitrobenzosulfonic acid. The charged liposomes demonstrated better physical stability than the neutral liposomes. The percentages of TA entrapped in all liposome formulations varied between 13.2 and 15.6%, and were independent of TA concen...
Biochimica et Biophysica Acta (BBA) - Biomembranes, 2003
Novel formulations of the halogenated corticosteroid, triamcinolone-acetonide, based on ultradeformable mixed lipid vesicles, TransfersomesR, are described. Their performance was tested in vivo using radioactive label measurements, to study the drug biodistribution, and murine ear edema, to determine the drug bioactivity. Sparse use of drug-loaded TransfersomesR on the skin ensures an almost exclusive delivery of triamcinolone-acetonide into the organ, thus arguably increasing the treatment safety. Delivery of triamcinolone-acetonide in the skin with ultradeformable vesicles prolongs the anti-inflammatory drug action several times compared to drug usage in a conventional crème or an ointment, the robustness of biological response for the former being at least identical to the latter. The required dose of TransfersomeRbased triamcinolone-acetonide is also greatly reduced. The drug dose of 0.2 Ag cm À 2 suppresses 75% of arachidonic acid-induced murine ear edema for at least 48 h. In contrast, a conventional formulation of triamcinolone-acetonide requires a 10-fold higher drug dosage to achieve a similar effect. In either case, increasing the applied corticosteroid amount delays the onset of anti-edema action.
IJPSM, 2021
Psoriasis is a chronic condition that is caused by the negative signals given by immune system, which leads to hyperproliferation and other inflammatory reactions on the skin. These conditions may adversely affect the quality of the patient's life leading to psychological stress. Topical delivery of drug is always preferred for Psoriasis because other treatments may lead to systemic intoxication and other adverse reactions. Triamcinolone is a topical corticosteroid belonging to BCS class IV (low solubility and permeability) used to treat Psoriasis. The limitations with transdermal delivery is that only a small amount of the drug can be transferred through the skin tissue due to the barrier effects of the Stratum corneum. Therefore, Novel transdermal delivery system, Cubosomes belonging to Nanostructured lipid carriers were chosen to overcome the issues of solubility and permeability. Twelve formulations were prepared with various ratios of Glyceryl monooleate (2.5 to 5%) & Poloxamer 407 (0.5 to 2%) and the formulations were evaluated for particle size, PDI, zeta potential, entrapment efficacy, drug content and in-vitro release. The best composition of Cubosomes was selected and incorporated into transdermal patch and the formulated patches were evaluated.
Liposomal Formulation for Dermal and Transdermal Drug Delivery: Past, Present and Future
Recent Patents on Drug Delivery & Formulation, 2008
Although the formulation of effective topical drug delivery system is one of the most sophisticated pharmaceutical preparations, it has attracted researchers due to many medical advantages associated with it. Topical drug delivery systems can act superficially on skin surface, locally in dermal layer of the skin or transdermally to provide successful delivery of drug molecules to the systemic circulation avoiding the traditional problems and limitations of conventional routes of drug delivery. Many novel formulations have been utilized topically to enhance either permeability or drug targeting to a specific layer of the skin such as Liposomes, ethosomes, transfersomes, niosomes and catezomes. The main problem with all of these formulations is that there is no distinct barrier between the targeting and localization action to a certain layer of the skin and the transdermal action to the circulation of these preparations. Any minimal change in the formulation could transform it from a local targeting preparation to a systemic one. This article deals with the innovations pertaining to the use of various types of liposomal preparations and liposomal like preparations for topical drug delivery and the patents associated with it.
Liposomal Gels as Carriers for Safer Topical Delivery of Tazarotene
The aim is to design a liposomal delivery system for topical administration of tazarotene capable of providing controlled and localized release of the encapsulated drug in order to minimize adverse effects associated with its topical use. Tazarotene loaded liposomes were prepared and characterized for entrapment efficiency, particle size and stability. Tazarotene liposomal gels were formulated and evaluated comparatively with commercial gel with respect to primary skin irritation and skin permeation. The effect of vesicular incorporation of tazarotene on its accumulation into hairless rat skin from liposomal suspension and gels were studied. The results of the study showed that the maximum entrapment efficiency recorded (93.49%±0.25) was achieved by formula having 1:1 lipoid S 100 to cholesterol molar ratio. The mean particle size of liposomal formulae ranged from (5.68µm-0.72µm). The stability profile of the selected system assessed for 90 days at refrigerated temperature showed no sign of sedimentation or color change with (86.27% ±0.44) of drug retained. All liposomal suspension and gels revealed higher drug retention compared to commercial gel, lesser skin irritancy and greater skin tolerance was also observed.