Effect of lipid and edge activator concentration on development of aceclofenac-loaded transfersomes gel for transdermal application: <i>in vitro</i> and <i>ex vivo</i> skin permeation

Dudhipala, Narendar; Mohammed, Riyaz Phasha; Youssef, Ahmed Adel Ali; Banala, Nagaraj

doi:10.1080/03639045.2020.1788069

Cited by 69 publications

(28 citation statements)

References 36 publications

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“…As the concentration of PCs increases, the high EE is achieved [ 55 ]. The concentration of PC determines the entrapment efficiency of drug in transfersomes [ 56 ]. The EE of VS-1 and VT-1 was greater than rest of the formulations.…”

Section: Discussionmentioning

confidence: 99%

Improved Bioavailability of Ebastine through Development of Transfersomal Oral Films

et al. 2021

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The main objective of this research work was the development and evaluation of transfersomes integrated oral films for the bioavailability enhancement of Ebastine (EBT) to treat allergic rhinitis. The flexible transfersomes, consisting of drug (EBT), lipid (Phosphatidylcholine) and edge activator (EA) Polyoxyethylene sorbitan monooleate or Sorbitan monolaurate, were prepared with the conventional thin film hydration method. The developed transfersomes were further integrated into oral films using the solvent casting method. Transfersomes were evaluated for their size distribution, surface charge, entrapment efficiency (EE%) and relative deformability, whereas the formulated oral films were characterized for weight, thickness, pH, folding endurance, tensile strength, % of elongation, degree of crystallinity, water content, content uniformity, in vitro drug release and ex vivo permeation, as well as in vivo pharmacokinetic and pharmacodynamics profile. The mean hydrodynamic diameter of transfersomes was detected to be 75.87 ± 0.55 nm with an average PDI and zeta potential of 0.089 ± 0.01 and 33.5 ± 0.39 mV, respectively. The highest deformability of transfersomes of 18.52 mg/s was observed in the VS-3 formulation. The average entrapment efficiency of the transfersomes was about 95.15 ± 1.4%. Transfersomal oral films were found smooth with an average weight, thickness and tensile strength of 174.72 ± 2.3 mg, 0.313 ± 0.03 mm and 36.4 ± 1.1 MPa, respectively. The folding endurance, pH and elongation were found 132 ± 1, 6.8 ± 0.2 and 10.03 ± 0.4%, respectively. The ex vivo permeability of EBT from formulation ETF-5 was found to be approximately 2.86 folds higher than the pure drug and 1.81 folds higher than plain film (i.e., without loaded transfersomes). The relative oral bioavailability of ETF-5 was 2.95- and 1.7-fold higher than that of EBT-suspension and plain film, respectively. In addition, ETF-5 suppressed the wheal and flare completely within 24 h. Based on the physicochemical considerations, as well as in vitro and in vivo characterizations, it is concluded that the highly flexible transfersomal oral films (TOFs) effectively improved the bioavailability and antihistamine activity of EBT.

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Section: Discussionmentioning

confidence: 99%

Improved Bioavailability of Ebastine through Development of Transfersomal Oral Films

et al. 2021

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“…Data for regression analysis were processed using the statistical function of Microsoft ® (MS) office excel (Office365, 2019, USA). To study the mechanism of drug release from NE, Zero-order, First-order, Higuchi, and Korsmeyer-Peppas equations [67,68] were chosen as mathematical models to characterize the in vitro release profile. These models are commonly used to describe the drug release pattern from drug delivery systems when the drug release mechanism is not clear or when there is more than one type of release phenomenon involved.…”

Section: In Vitro Release Studiesmentioning

confidence: 99%

Design of Topical Ocular Ciprofloxacin Nanoemulsion for the Management of Bacterial Keratitis

et al. 2021

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Bacterial keratitis (BK) is a critical ocular infection that can lead to serious visual disability. Ciprofloxacin (CIP), moxifloxacin (MOX), and levofloxacin (LFX) have been accepted as monotherapies by the US Food and Drug Administration for BK treatment. CIP is available commercially at 0.3% w/v concentration as an ophthalmic solution and as an ointment for ocular delivery. Because of solubility issues at physiological pH, CIP precipitation can occur at the corneal surface post instillation of the solution dosage form. Consequently, the ocular bioavailability of CIP is reduced. The ointment dosage form is associated with side effects such as blurred vision, itching, redness, eye discomfort, and eye dryness. This study aimed to design a CIP loaded nanoemulsion (NE; CIP-NE) to facilitate drug penetration into the corneal layers for improved therapeutic outcomes as well as to overcome the drawbacks of the current commercial ophthalmic formulations. CIP-NE formulations were prepared by hot homogenization and ultrasonication, using oleic acid (CIP-O-NE) and Labrafac® Lipophile WL 1349 (CIP-L-NE) as the oily phase, and Tween® 80 and Poloxamer 188 as surfactants. Optimized CIP-NE was further evaluated with respect to in vitro release, ex vivo transcorneal permeation, and moist heat sterilization process, using commercial CIP ophthalmic solution as a control. Optimized CIP-O-NE formulation showed a globule size, polydispersity index, and zeta potential of 121.6 ± 1.5 nm, 0.13 ± 0.01, and −35.1 ± 2.1 mV, respectively, with 100.1 ± 2.0 % drug content and was spherical in shape. In vitro release and ex vivo transcorneal permeation studies exhibited sustained release and a 2.1-fold permeation enhancement, respectively, compared with commercial CIP ophthalmic solution. Autoclaved CIP-O-NE formulation was found to be stable for one month (last time-point tested) at refrigerated and room temperature. Therefore, CIP-NE formulation could serve as an effective delivery system for CIP and could improve treatment outcomes in BK.

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“…To create a balance between biological qualities and biological uses, as well as the route of administration, the pH level of compositions must be suitable. The lipid of transferosomes is similar to the phospholipid layer of a cell membrane, and unionised medicines are last membrane phospholipid bilayer and enter the c intracellular route [27,28].…”

Section: Of Hydration Mediummentioning

confidence: 99%

Review on Transferosomes and Transferosomal Gels

Kumar

2021

JPRI

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Transdermal drug delivery systems (TDDS), which are self-administrable and non-invasive, can improve bioavailability and patient compliance by bypassing first-pass metabolism. Vesicular-based TDDS have attracted a lot of attention in recent years because they're designed for controlled, efficient, and targeted drug delivery. One of these delivery technologies, transferosomal-based formulations, has grown in popularity due to its ability to achieve all of the desired criteria and quality qualities. Transferosomes combine the characteristics of liposomes and niosomes because they contain both liposomes (phospholipids and cholesterols) and niosomes as components (nonionic surfactants; edge activators). as a result, they are referred to as the first generation of elastic liposomes. However transdermal drug delivery is difficult due to the presence of the skin's protective barrier, transferosomal drug delivery overcomes all obstacles due to its unique characteristics, such as its ultradeformable vesicular nature. The benefits, limitations, modes of penetration, formulations, production and assessment methodologies, and pharmaceutical uses of transferosomal drug delivery systems are discussed in this paper. Conclusion: Transferosomes have several importance over other vesicular systems, including greater deformability, greater penetration power across skin, the ability to deliver systemic drugs, and higher stability.

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Effect of lipid and edge activator concentration on development of aceclofenac-loaded transfersomes gel for transdermal application: in vitro and ex vivo skin permeation

Cited by 69 publications

References 36 publications

Improved Bioavailability of Ebastine through Development of Transfersomal Oral Films

Improved Bioavailability of Ebastine through Development of Transfersomal Oral Films

Design of Topical Ocular Ciprofloxacin Nanoemulsion for the Management of Bacterial Keratitis

Review on Transferosomes and Transferosomal Gels

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