Formulation and Penetration Testing of Ethosome Azelaic Acid on Abdominal Skin White Male Rats (Rattus Norvegicus) With Franz Diffusion Cell

Nurleni, Novi; Iskandarsyah, Iskandarsyah; Aulia, Ahmad

doi:10.22159/ajpcr.2018.v11i4.22193

Cited by 8 publications

(9 citation statements)

References 8 publications

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“…One milliliter of transferosome was added to 1 mL of Triton X (0.1%) and centrifuged at 10,000 rpm for 1 h (4°C) to allow the separation of the total drug. After removal of the supernatant, the supernatant was added to methanol and then analyzed by highpressure liquid chromatography (HPLC) at 204 nm using an HPLC system (Shimadzu, Jepang) [11]. The %EE of MIC in the prepared transferosome was calculated applying the following equation:…”

Section: Transferosome Entrapment Efficiency (%Ee) Of Lynestrenolmentioning

confidence: 99%

Effects of Sonication on Size Distribution and Entrapment of Lynestrenol Transferosome

2020

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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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Section: Transferosome Entrapment Efficiency (%Ee) Of Lynestrenolmentioning

confidence: 99%

Effects of Sonication on Size Distribution and Entrapment of Lynestrenol Transferosome

2020

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“…The PDI value should be <0.5. The degree of heterogeneity of particlesize distribution is lower when the PDI value is closer to zero [17]. The PDI values of F2, F3, and F4 ethosomes were higher than 0.5 (Table 3) which indicated rather polydisperse (heterogeneous) suspensions and poor particle-size distribution; particle-size distribution curves with abnormal distributions and more than one peak.…”

Section: Particle-size Distribution and Zeta Potentialmentioning

confidence: 94%

“…The elliptical form can be caused by the high concentration of ethanol which increases membrane fluidity. Cholesterol can be added to decrease the fluidity [15][16][17][18] and produce more spherical vesicles. Spherical SUVs were found inside multilamellar vesicles due to sonication, which may have disturbed the multilamellar structure and created unilamellar vesicles [19].…”

Section: Morphologymentioning

confidence: 99%

Preparation and Characterization of Anti-Acne Ethosomes Using Cold and Thin-Layer Hydration Methods

Mustofa

Iskandarsyah

2018

Int J App Pharm

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Objective: This study aimed to prepare and characterize anti-acne ethosomes using the cold-and thin-layer hydration methods.Methods: A sonication step was included during ethosome preparation to improve the quality of the cold method. Azelaic acid, Phospholipon 90G, ethanol, propylene glycol, and phosphate buffer (pH 7.4) were used in the procedures. Prepared ethosomal suspensions were characterized using transmission electron microscopy, particle-size analysis, and spectrophotometry.Results: Ethosomes prepared using the thin-layer hydration method (F1) had small unilamellar vesicles, while those prepared using the cold method with 15-min sonication (F4) showed spherical, elliptical, unilamellar, and multilamellar vesicles. F1 ethosomes had a D mean volume of 648.57±231.26, whereas those prepared using the cold method with 5-(F2), 10-(F3), and 15-min (F4) sonication had D mean volumes of 2734.04±231.49 nm, 948.90±394.52 nm, and 931.69±471.84 nm, respectively. Polydispersity indices of F2, F3, and F4 ethosomes were 0.74±0.21, 0.86±0.05, and 0.91±0.03, respectively, with a poor particle-size distribution, compared to that of F1 (0.39±0.01). Zeta potentials of F1-F4 ethosomes were −38.27±1.72 mV, −23.53±1.04 mV, −31.4±1.04 mV, and −34.3±1.61 mV, respectively. Entrapment efficiencies of F1-F4 ethosomes were 90.71±0.11%, 53.84±3.16%, 72.56±0.28%, and 75.11±1.42%, respectively. Conclusion:Anti-acne ethosomes produced using the thin-layer hydration method had superior properties than those produced using the cold method with 15-min sonication.

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“…All experiments were performed in triplicate and the mean values were calculated. The percentage cumulative penetration per square centimeter of gel was plotted against time for each formulation [14,15].…”

Section: In Vitro Diffusion Testsmentioning

confidence: 99%

In Vitro Study of a Transfersomal Gel Preparation Containing Lynestrenol as a Transdermal Drug Delivery System

2020

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Objective: Lynestrenol, a progestin hormone derivative, can suppress the productions of endogenous estrogen and progesterone hormones (ovaries)to prevent ovulation. In this study, lynestrenol was included in various transfersomal gel preparations for its transdermal delivery into fat (F)-andnon-fat (NF)-containing skin tissues.Methods: Lynestrenol transfersome vesicles were prepared by encapsulating the drug in varied concentrations of phosphatidylcholine and Tween80 using lipid film hydration method. Transfersomes were produced in the form of gel preparations at a dose of 0.15 mg/week and evaluated fortheir particle size, percentage of entrapment efficiency, and particle polydispersity. We performed in vitro evaluations of the formulation variants F0(lynestrenol gel control) and F1 and F2 (lynestrenol transfersome gels) with variations in their phosphatidylcholine and Tween 80 content. We thenperformed an in vitro evaluation using the Franz diffusion cell (FDC) method for 12 h using all three formulations on F and NF-containing rat skin.Results: The FDC results demonstrated that lynestrenol was deposited into fat tissue and increased concentrations of Tween 80 (edge activator)increased lynestrenol delivery into this tissue. In addition, the percentages of drug penetration from NF rat skin treated with F0, F1, and F2 gels were19.56%, 20.13%, and 20.56%, respectively, and those from F rat skin were 17.16%, 17.38%, and 17.50%, respectively.Conclusion: In vitro evaluation using the FDC method indicates that transdermal drug delivery through to fat tissues using transfersomes is apromising method for lynestrenol delivery.

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Formulation and Penetration Testing of Ethosome Azelaic Acid on Abdominal Skin White Male Rats (Rattus Norvegicus) With Franz Diffusion Cell

Cited by 8 publications

References 8 publications

Effects of Sonication on Size Distribution and Entrapment of Lynestrenol Transferosome

Effects of Sonication on Size Distribution and Entrapment of Lynestrenol Transferosome

Preparation and Characterization of Anti-Acne Ethosomes Using Cold and Thin-Layer Hydration Methods

In Vitro Study of a Transfersomal Gel Preparation Containing Lynestrenol as a Transdermal Drug Delivery System

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