Pharmacokinetic and pharmacodynamic studies of etodolac loaded vesicular gels on rats by transdermal delivery

Madhavi, Nimmathota; Sudhakar, Beeravelli; Reddy, K.T. Ramakrishna; Ratna, J. Vijaya

doi:10.1007/s40199-018-0214-4

Cited by 9 publications

(5 citation statements)

References 26 publications

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“…Conventional gel formulations with penetration enhancers were reported to provide an efficient therapy [6]. Besides this, novel drug delivery systems such as nanosuspensions [4,7], microemulsions [8], vesicular carriers [9,10], and lipid nanoparticles [11] were designed to provide an efficient ETO delivery via transdermal route. Another option could be the conventional rectal suppositories [12] and in situ gelling liquid suppositories [3].…”

Section: Introductionmentioning

confidence: 99%

Preparation and characterization studies of etodolac suppositories: investigation on oleaginous blends of Witepsol® H15

ÖZDEMİR¹,

Uner²,

KARAKÜÇÜK³

2023

jrp

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Etodolac is a non-steroidal anti-inflammatory drug that is categorized as a BCS class-II drug due to its low aqueous solubility and high permeability. Frequent dosing, extensive liver metabolism, and low dissolution rates are major limitations of etodolac. The present study focuses on the designing of novel suppository base blends for providing an effective delivery of etodolac. The oils (Caprylic/capric triglyceride, isopropyl isostearate, and isopropyl palmitate) were added to Witepsol ® H15 to form suppository base blends. White, odorless, and torpedo-shaped suppositories were developed by using two parts of Witepsol ® H15 and one part of the oil. All of the suppositories prepared with different blends were found uniform in weight and content. The mechanical strength of all suppositories was in an acceptable range for suppositories (2.0 -3.8 kg/cm 2 ). The suppositories showed a disintegration time between 13 and 19 minutes. First-order release kinetics were observed after the in vitro release studies. The suppository base blends released 85%-90% of etodolac in the first hour while 60% of etodolac was released from Witepsol ® H15 base alone. Prolonged drug release was achieved after 2 hours all of the formulations reached the plateau levels. The oil blends exhibited higher release percentages (96% -99%) than plain Witepsol ® H15 base (89%). Therefore novel suppository base blends could be a promising formulation ingredient for the etodolac suppositories.

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Section: Introductionmentioning

confidence: 99%

Preparation and characterization studies of etodolac suppositories: investigation on oleaginous blends of Witepsol® H15

ÖZDEMİR¹,

Uner²,

KARAKÜÇÜK³

2023

jrp

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“…Besides, conventional topical formulations possess poor penetration to skin barriers, therefore previous literature reported the application of novel drug delivery systems to potentiate safety and efficacy of topical formulations of etodolac. These systems comprise blend of lipids, permeation enhancers and edge activators, which propagate the permeation, such as Liposomes 17 , Solid lipid nanoparticles (SLNs) 18 , Nano lipoidal carriers (NLCs) 19 , Cubosomes 20 , Film-forming spray 21 , Ethosomes 22 , Transferosomes 23 , Nanosponges hydrogel 24 , Niosomes 14 , Transethosomes 25 , Nanosuspension 26 and Hydrophilic gel 13 . The inclusion of the edge activators, i.e., tween 20, tween 80, tween 60, span 60 and sodium deoxycholate (SDC) etc., have been found to improve the deformation ability of lipid-based systems after topical application.…”

Section: Introductionmentioning

confidence: 99%

Exploring the therapeutic potential of sodium deoxycholate tailored deformable-emulsomes of etodolac for effective management of arthritis

Sharma,

Mahajan,

Thakur

et al. 2023

Sci Rep

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The current piece of research intends to evaluate the potential of combining etodolac with deformable-emulsomes, a flexible vesicular system, as a promising strategy for the topical therapy of arthritis. The developed carrier system featured nanometric dimensions (102 nm), an improved zeta potential (− 5.05 mV), sustained drug release (31.33%), and enhanced drug deposition (33.13%) of DE-gel vis-à-vis conventional system (10.34% and 14.71%). The amount of permeation of the developed nano formulation across skin layers was demonstrated through CLSM and dermatokinetics studies. The safety profile of deformable-emulsomes has been investigated through in vitro HaCaT cell culture studies and skin compliance studies. The efficacy of the DE-gel formulation was sevenfold higher in case of Xylene induced ear edema model and 2.2-folds in CFA induced arthritis model than that of group treated with conventional gel (p < 0.01). The main technological rationale lies in the use of phospholipid and sodium deoxycholate-based nanoscale flexible lipoidal vesicles, which effectively encapsulate drug molecules within their interiors. This encapsulation enhances the molecular interactions and facilitates the transportation of the drug molecule effectively to the target-site. Hence, these findings offer robust scientific evidence to support additional investigation into the potential utility of flexible vesicular systems as a promising drug delivery alternative for molecules of this nature.

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“…Recently, local delivery systems with ETD have gained particular attention with potential to enhance local treatment efficacy and simultaneously reduce systemic adverse effects. ETD is a biopharmaceutical classification system (BCS) class II drug, characterized by poor solubility in water (0.016 mg/mL), but high permeability through a lipophilic barriers (log P 2.5) [ 1 , 2 , 3 , 4 , 5 , 6 , 7 ]. To reduce the adverse effect of ETD and to obtain high drug concentration, polymer coatings, carriers that ensure extended release or alternative drug administration route are developed [ 5 , 6 ].…”

Section: Introductionmentioning

confidence: 99%

“…In recent decades, transdermal drug delivery has become a novel strategy as it can improve patient compliance (pain-free and safe application), reduce frequency of administration (elimination of first-pass effect, protection from drug demotion), and provide reduction of side effects [ 6 , 7 ]. It should be stated that one topical preparation (Proxym ® ) is commercially available which is a combined product with several biologically active agents including camphor 4%, linseed oil 3%, menthol 10%, and methyl salicylate 5%.…”

Section: Introductionmentioning

confidence: 99%

“…Still there is no topical formulation containing only ETD. A number of research papers have recently drawn attention to the application for topical delivery of ETD, including hydrogel [ 8 ], niosomal gel [ 5 ], nanosponges [ 9 ], liposomes [ 10 ], ethosomes [ 6 ] and organogel [ 11 ]. Nanocrystals, liposomes, nanoemulsions, and lipid nanoparticles have shown promising benefits as modern nanocarriers [ 12 ].…”

Section: Introductionmentioning

confidence: 99%

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Nanostructured Lipid Carriers Engineered as Topical Delivery of Etodolac: Optimization and Cytotoxicity Studies

et al. 2021

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Etodolac (ETD), a nonsteroidal anti-inflammatory drug, exhibits antinflammatory, analgesic, and antipyretic activity. The main type of ETD administration is oral route, which is associated with significant systemic side effects. Nanostructured lipid carriers (NLC), a modern lipid formulation, are non-toxic, biocompatible, can improve the solubility and stability of drugs. Nanostructured lipid carriers (NLC) containing etodolac were prepared by a melt-emulsification and ultrasonication technique. Full factorial design (FFD) was applied to optimize the composition of NLC and their properties such as zeta potential, polidyspersity index, and entrapment efficiency. Formulations consisting of Capryol 90, glicerol monostearate, and Tween 20 displayed particle size below 300 nm, encapsulated drug with efficiency of approximately 87% and prolonged drug release up to 24 h. Stable formulations displayed moderately negative surface charge suggesting their limited ability to interact with skin surface but simultaneously presenting their lower risk to cause cell-membrane disruption. In fact, cytotoxicity assessment using human dermal fibroblasts and human epidermal keratinocytes revealed that etodolac-loaded NLC had no important impact on skin cells viability evaluated in vitro, which might evidence that NLC formulations are safe for dermal delivery. The studies developed were relatively fast and simple, requiring no specialized equipment method to prepare NLC as ETD carriers ensuring better solubility and prolonged drug release.

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Pharmacokinetic and pharmacodynamic studies of etodolac loaded vesicular gels on rats by transdermal delivery

Abstract: The pharmacokinetic and pharmacodynamic studies indicated that the vesicular gels show better results compared to PROXYM®. The correlation coefficient value between PK and PD was found to be 0.9635. Graphical abstract ᅟ.

Cited by 9 publications

References 26 publications

Preparation and characterization studies of etodolac suppositories: investigation on oleaginous blends of Witepsol® H15

Preparation and characterization studies of etodolac suppositories: investigation on oleaginous blends of Witepsol® H15

Exploring the therapeutic potential of sodium deoxycholate tailored deformable-emulsomes of etodolac for effective management of arthritis

Nanostructured Lipid Carriers Engineered as Topical Delivery of Etodolac: Optimization and Cytotoxicity Studies

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