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Pharmaceutics ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1968
Author(s):  
Renata Basto ◽  
Raquel Andrade ◽  
Cláudia Nunes ◽  
Sofia A. Costa Lima ◽  
Salette Reis

Niacinamide (NIA) has been widely used in halting the features of ageing by acting as an antioxidant and preventing dehydration. NIA’s physicochemical properties suggest difficulties in surpassing the barrier imposed by the stratum corneum layer to reach the target in the skin. To improve cutaneous delivery of NIA, a hybrid nanogel was designed using carrageenan and polyvinylpyrrolidone polymers combined with jojoba oil as a permeation enhancer. Three different types of transethosomes were prepared by the thin-film hydration method, made distinct by the presence of either an edge activator or a permeation enhancer, to allow for a controlled delivery of NIA. Formulations were characterized by measurements of size, polydispersity index, zeta potential, encapsulation efficiency, and loading capacity, and by evaluating their chemical interactions and morphology. Skin permeation assays were performed using Franz diffusion cells. The hybrid hydrogels exhibited robust, porous, and highly aligned macrostructures, and when present, jojoba oil changed their morphology. Skin permeation studies with transethosomes-loaded hydrogels showed that nanogels per se exhibit a more controlled and enhanced permeation, in particular when jojoba oil was present in the transethosomes. These promising nanogels protected the human keratinocytes from UV radiation, and thus can be added to sunscreens or after-sun lotions to improve skin protection.


2021 ◽  
Vol 3 (2) ◽  
pp. 78-86
Author(s):  
Gabena Indrayani Dalimunthe ◽  
Ricky Andi Ayaputra

Diclofenac sodium is a Transfersom is a transdermal delivery system consisting of phospholipids and edge activators. Transfersom increases the size of the stratum corneum lipid barrier pores, then enters the skin through the drive of the trans-barrier motion and squeezes itself to follow the lipid barrier pore size. The purpose of this study is to determine the effect of the tween-80 concentration as an edge activator on the characteristics and diffusion rate of diclofenac sodium transfersom. Transferom preparation used the vortex-sonication method which was made in five formulae with variations in the concentration ratio of phosphatidylcholine and tween-80 (95:05, 90:10, 85:15, 80:20, and 75:25). The results show that all five formulae have different morphological forms. The results of statistical tests using One-Way ANOVA finds a significant effect (p-value) of the edge activator concentration on the diffusion rate of diclofenac sodium transfersom.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1749
Author(s):  
Imran Kazmi ◽  
Fahad A Al-Abbasi ◽  
Muhammad Shahid Nadeem ◽  
Hisham N Altayb ◽  
Sultan Alshehri ◽  
...  

In the present study, luteolin (LT)-loaded nanosized vesicles (LT-NVs) were prepared by a solvent evaporation–hydration method using phospholipid and edge activator. The formulation was optimized using three factors at a three-level Box–Behnken design. The formulated LT-NVs were prepared using the three independent variables phospholipid (A), edge activator (B) and sonication time (C). The effect of used variables was assessed on the vesicle size (Y1) and encapsulation efficiency (Y2). The selection of optimum composition (LT-NVopt) was based on the point prediction method of the software. The prepared LT-NVopt showed the particle size of 189.92 ± 3.25 nm with an encapsulation efficiency of 92.43 ± 4.12% with PDI and zeta potential value of 0.32 and −21 mV, respectively. The formulation LT-NVopt was further converted into Carbopol 934 gel (1% w/v) to enhance skin retention. LT-NVoptG was further characterized for viscosity, spreadability, drug content, drug release, drug permeation and antioxidant, antimicrobial and cytotoxicity assessment. The evaluation result revealed optimum pH, viscosity, spreadability and good drug content. There was enhanced LT release (60.81 ± 2.87%), as well as LT permeation (128.21 ± 3.56 µg/cm2/h), which was found in comparison to the pure LT. The antioxidant and antimicrobial study results revealed significantly (p ˂ 0.05) better antioxidant potential and antimicrobial activity against the tested organisms. Finally, the samples were evaluated for cytotoxicity assessment using skin cancer cell line and results revealed a significant difference in the viability % at the tested concentration. LT-NVoptG showed a significantly lower IC50 value than the pure LT. From the study, it can be concluded that the prepared LT-NVoptG was found to be an alternative to the synthetic drug as well as conventional delivery systems.


Author(s):  
Sachin Rathod ◽  
Shristi Arya ◽  
Rahul Shukla ◽  
Debes Ray ◽  
Vinod K. Aswal ◽  
...  

2020 ◽  
Vol 2 (3) ◽  
Author(s):  
Luthfia Azzahra ◽  
Soraya Ratnawulan Mita ◽  
Sriwidodo Sriwidodo

Herbal compounds have different physicochemical properties. Its use on the oral route often has low biological availability. Therefore, alternative transdermal routes are used through the skin. The stratum corneum skin layer is the most difficult layer to penetrate. Therefore it is necessary to use a drug delivery system such as ethosome, transfersome or transethosome to increase transdermal drug delivery. This review article aims to look at the potential of ethosome, transfersome, and transethosome in increasing their ability to deliver herbal drugs in terms of their formulation and characterization. Literature searches were performed using online search engines namely NCBI and Google Scholar with the keywords ‘Transdermal Drug Delivery System’, 'Ethosome', 'Transfersome', and 'Transethosome'. The result showed compositions of ethosomes are phospholipids, water, and ethanol. The composition of transfersome is phospholipid, water, and edge activator. Transethosomes are a combination of phospholipids, water, ethanol, and edge activators. The role of ethanol and edge activator is thought to increase skin permeation. Transdermal drug delivery systems can be used on herbal drugs to increase transdermal drug delivery.Keywords: Transdermal, Ethosome, Transfersome, Transethosome, Herbal.


2020 ◽  
Vol 11 (12) ◽  
pp. 807-819
Author(s):  
Nirmala Nayak ◽  
Preethi Somanna ◽  
Amit B Patil ◽  
Arun Radhakrishnan

Psoriasis is a chronic autoimmune condition that is described by infected skin patches. Ultradeformable vesicles have been a novel carrier for the treatment of psoriasis in topical and transdermal therapy. The systemic route may induce adverse effects and the drug concentration may not be localized when applied topically to the psoriasis skin due to their physicochemical properties. These limitations can be overcome by a vesicular delivery system such as transferosomes. Research on transferosomes is ongoing. Transferosomes are flexible deformable vesicular structures, which consist of a bilayer softening agent such as an edge activator, which allows it to penetrate deeper dermal layers. This review outlines the use of transferosomes in the treatment of deeply rooted dermal disorders like psoriasis.


2020 ◽  
Vol 26 ◽  
Author(s):  
Drashti Patel ◽  
Bappaditya Chatterjee

: Transfersomes are bilayer vesicles composed of phospholipid and edge-activators, which are mostly surfactant. Transfersomes based drug delivery system has gained a lot of interest of the pharmaceutical researchers for their ability to improve drug penetration and permeation through the skin. Transdermal drug delivery via transfersomes has the potential to overcome the challenge of low systemic availability. However, this complex vesicular system has different issues to consider for developing a successful transdermal delivery system. One of the major ingredients, phospholipid has versatile sources and variable effect on the vesicle size and drug entrapment in transfersomes. The other one termed as edge-activator or surfactant has some crucial consideration of skin damage and toxicity depending upon its type and concentration. A complex interaction between type and concentration of phospholipid and surfactant was observed, which affect the physicochemical properties of transfersomes. This review focuses on the practical factors related to these two major ingredients such as phospholipid and surfactant. The origin, purity, desired concentration, the susceptibility of degradation, etc. are the important factors for selecting phospholipid. Regarding surfactants, the major aspects are type and desired concentration. A successful development of transfersomes based drug delivery system depends on the proper considerations of these factors and practical aspects.


Nanomaterials ◽  
2020 ◽  
Vol 10 (7) ◽  
pp. 1270
Author(s):  
Osama A. A. Ahmed ◽  
Usama A. Fahmy ◽  
Shaimaa M. Badr-Eldin ◽  
Hibah M. Aldawsari ◽  
Zuhier A. Awan ◽  
...  

Flibanserin (FLB) is a nonhormonal medicine approved by the Food and Drug Administration (FDA) to treat the hypoactive sexual appetite disorder in females. However, the peroral administration of the medicine is greatly affected by its poor bioavailability as a result of its extensive first-pass effect and poor solubility. Aiming at circumventing these drawbacks, this work involves the formulation of optimized FLB transfersome (TRF) loaded intranasal hydrogel. Box–Behnken design was utilized for the improvement of FLB TRFs with decreased size. The FLB-to-phospholipid molar ratio, the edge activator hydrophilic lipophilic balance, and the pH of the hydration medium all exhibited significant effects on the TRF size. The optimized/developed TRFs were unilamellar in shape. Hydroxypropyl methyl cellulose based hydrogel filled with the optimized FLB TRFs exhibited an improved ex vivo permeation when compared with the control FLB-loaded hydrogel. In addition, the optimized TRF-loaded hydrogel exhibited higher bioavailability and enhanced brain delivery relative to the control hydrogel following intranasal administration in Wistar rats. The results foreshadow the possible potential application of the proposed intranasal optimized FLB-TRF-loaded hydrogel to increase the bioavailability and nose-to-brain delivery of the drug.


Author(s):  
ISKANDARSYAH ISKANDARSYAH ◽  
CAMELIA DWI PUTRI MASRIJAL ◽  
HARMITA HARMITA

Objective: The aim of this study was to develop transferosome vesicles for the transdermal drug delivery of lynestrenol.Methods: The lynestrenol transferosome vesicle was made by encapsulating the drug in a variation of phosphatidylcholine and Tween 80 by the thinlayerhydration method. The resulting transferosome vesicles were modified with a time variation of 30, 60, 90, and 120 min, and sonication variationswere paused and not paused. Particle size evaluation, polydispersity (PDI), and entrapment efficiency (%EE) were carried out on the variation ofsonication time.Results: The evaluation results showed that sonication without pauses showed better %EE and particle size than sonication with pauses andincreasing concentration of Tween 80 (edge activator). The %EE increased, and particle size decreased with increasing sonication time; PDI of vesicleswas heterogeneous with increasing sonication time. The %EE in formulas F1 and F2 after 120 min was 73.06% and 76.06% (paused) and 80.40% and82.97% (without paused). The particle size of formula F1 and F2 after 120 min 575.4 nm and 471.6 nm (paused) and 524.1 nm and 434.7 nm (withoutpaused). The PDI formulas of F1 and F2 after 120 min were 0.69 and 0.763 (paused) and 0.84 and 0.59 (without paused).Conclusion: Based on the results of the transferosome vesicle characteristics, it was shown that the optimal vesicle composition for packaginglynestrenol was vesicles that were composed of phosphatidylcholine and Tween 80 without pauses and could potentially be used as a transdermaldrug delivery system.


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