A Mixed Micellar Formulation for the Transdermal Delivery of an Indirubin Analog

Seo, Seol Hwa; Kim, Eunhwan; Joo, Yechan; Lee, Juseung; Oh, Kyung Taek; Hwang, Sung Joo; Choi, Kang Yell

doi:10.3390/pharmaceutics12020175

Cited by 19 publications

(12 citation statements)

References 37 publications

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“…Such surfactants include nonionic Kolliphors (known before as Cremophors) which are represented by Kolliphor ® ELP (ELP) and Kolliphor ® RH 40 (RH40). These surfactants are applied, among others, in pharmacy [ 8 , 9 ]. Their main constituent is triricinoleate ester of ethoxylated glycerol ( Scheme S1 in Supplementary Materials ).…”

Section: Introductionmentioning

confidence: 99%

Adsorption Properties and Composition of Binary Kolliphor Mixtures at the Water–Air Interface at Different Temperatures

2022

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The studies on the adsorption properties and composition of the adsorbed monolayer at the water–air interface of the binary Kolliphor® ELP (ELP) and Kolliphor® RH 40 (RH40) mixtures based on the measurements of the surface tension (γLV) of their aqueous solution in the temperature range from 293 to 318 K were carried out. The γLV isotherms were described by the exponential function of the second order and the Szyszkowski equation as well as predicted by Fainerman and Miller equation. The obtained γLV isotherms were analyzed using the exponential function of the second order, the Szyszkowski, Fainerman and Miller as well as independent adsorption equations. The γLV isotherms were also used for determination of the Gibbs surface excess concentration of RH40, ELP and their mixture (Γ) at the water–air interface as well as the mixed monolayer composition. Based on Γ and the constant a in the Szyszkowski equation, the standard thermodynamic functions of adsorption were considered. From the consideration dealing with the γLV isotherms obtained by us, it results, among others, that these isotherms for the non-ideal solution of macromolecular surfactants mixture can be predicted using the Fainerman and Miller equation. From this consideration, it also results that a simple method proposed by us, based on the isotherms of RH40 and ELP, allows us to predict the composition of their mixed monolayer in the whole concentration range of RH40 and ELP in the bulk phase.

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Section: Introductionmentioning

confidence: 99%

Adsorption Properties and Composition of Binary Kolliphor Mixtures at the Water–Air Interface at Different Temperatures

2022

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“…The Tween 80 has long-chain fatty acid and are available to decrease the interfacial tension between the nutmeg oil and cosurfactants, which provides clear Microemulsion (Handa et al, 2021). The PEG 400 molecule has two parallel helical bonds that form molecular complexes with active substances and cosurfactants in a circular chain formation to form intramolecular dispersions that can maintain stability of drug molecules (Seo et al, 2020). Both Tween 80 and PEG 400 could protect active ingredients from thermal and light exposure so that the microemulsion activity would be as stable as the physical appearance (Handa et al, 2021;Lv et al, 2018).…”

Section: Resultsmentioning

confidence: 99%

Chemical qualitative analysis and spf value stability of nutmeg seed oil in microemulsions with tween 80 and PEG 400 as surfactants and cosurfactants

Shabrina

Safitri

Fithria³

et al. 2022

Pharmaciana

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Nutmeg oil contains α-pinene, which can be used as sunscreen. The combination of Tween 80 and PEG 400 can maintain the stability of nutmeg oil microemulsion. This research was a follow-up study that aims to determine the stability of the SPF value and qualitative chemical content of nutmeg seed oil microemulsions (NSM). NSM was made with a nutmeg seed oil concentration of 6.4% and tween 80 and PEG 400 as surfactants and cosurfactants with variations in the ratio of F1 (5: 4), F2 (6: 4), and F3 (7: 4). Nutmeg seed oil and NSM content was analyzed using GC-MS. NSM formula were tested for in vitro SPF value stability by storing NSM in a climatic chamber at 30 °C ± 2 °C with RH 65 % ± 5 % for 4 weeks. The SPF values were calculated every week. GC-MS data were analyzed descriptively and data of SPF value stability were analyzed statistically using one-way ANOVA. The GC-MS results of nutmeg seed oil showed 35 components, including significant compounds, namely αpinene, sabinene, β-phellandrene and also α-terpinolene. GC-MS results of NSM showed those significant compounds were still detected after being formulated in microemulsion. The results of the sunscreen activity test of NSM before storage were 10.31 ± 0.03 (F1); 10.47 ± 0.07 (F2); 10.45 ± 0.03 (F3) and did not show significant change after storage for 4 weeks (p > 0.05). The SPF values of NSM were categorized in maximum activity.

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“…To validate the successful establishment of the insulin‐resistant mouse model, fasting glucose levels were assessed using a One Touch Ultra glucometer (LifeScan). Subsequently, each HFD‐fed mouse with fasting glucose levels higher than 7.0 mmol/L was orally administered KY19334 (25 mg/kg), sitagliptin (50 mg/kg, Selleckchem) or its vehicle 18 for 5 days at weeks 8 and 12. After the removal of the drugs, mice were maintained for 3 weeks on an HFD.…”

Section: Methodsmentioning

confidence: 99%

Inhibition of CXXC5 function reverses obesity‐related metabolic diseases

Seo

Kim

Lee³

et al. 2022

Clinical & Translational Med

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Background Metabolic diseases, including type 2 diabetes, have long been considered incurable, chronic conditions resulting from a variety of pathological conditions in obese patients. Growing evidence suggests the Wnt/β‐catenin pathway is a major pathway in adipose tissue remodelling, pancreatic β‐cell regeneration and energy expenditure through regulation of key metabolic target genes in various tissues. CXXC5‐type zinc finger protein 5 (CXXC5) is identified negative feedback regulator of the Wnt/β‐catenin pathway that functions via Dishevelled (Dvl) binding. Methods Expression level of CXXC5 was characterised in clinical samples and diabetes‐induced mice model. Diabetes‐induced mice model was established by using high‐fat diet (HFD). HFD‐fed mice treated with KY19334, a small molecule inhibiting CXXC5‐Dvl protein–protein interaction (PPI), was used to assess the role of CXXC5 in metabolic diseases. Results Here, we show that CXXC5 is overexpressed with suppression of Wnt/β‐catenin signalling in visceral adipose tissues of patients with obesity‐related diabetes. Meanwhile, Cxxc5 −/− mice fed an HFD exhibited resistance to metabolic dysregulation. KY19334 restores the lowered Wnt/β‐catenin signalling and reverses metabolic abnormalities as observed in HFD‐fed Cxxc5 −/− mice. Administration of KY19334 on HFD‐fed mice had a long‐lasting glucose‐controlling effect through remodelling of adipocytes and regeneration of pancreatic β‐cells. Conclusion Overall, the inhibition of CXXC5 function by small molecule‐mediated interference of Dvl binding is a potential therapeutic strategy for the treatment of obesity‐related diabetes.

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A Mixed Micellar Formulation for the Transdermal Delivery of an Indirubin Analog

Cited by 19 publications

References 37 publications

Adsorption Properties and Composition of Binary Kolliphor Mixtures at the Water–Air Interface at Different Temperatures

Adsorption Properties and Composition of Binary Kolliphor Mixtures at the Water–Air Interface at Different Temperatures

Chemical qualitative analysis and spf value stability of nutmeg seed oil in microemulsions with tween 80 and PEG 400 as surfactants and cosurfactants

Inhibition of CXXC5 function reverses obesity‐related metabolic diseases

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