Liposome and microemulsion loaded with ibuprofen: from preparation to mechanism of drug transport

Yuhang, Xu; Cai, Ye; Meng, Yun; Long, Wu; Chen, Jingbao; Cao, Weiguo; Chu, Xiaoqin

doi:10.1080/02652048.2022.2131920

Cited by 7 publications

(3 citation statements)

References 69 publications

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“…Second-generation TDDSs, with their chemical penetration enhancers and nanocarriers, increase the transdermal delivery of small molecules, and third-generation TDDSs, with their enhancement strategies, enable the successful transdermal delivery of various large molecules. In this section, we specifically describe the permeation enhancement strategies of second-and third-generation TDDSs 58 , and we summarize their advantages, limitations, and transdermal delivery mechanisms, as indicated in Table 2 59 , 60 , 61 , 62 , 63 , 64 , 65 , 66 , 67 , 68 , 69 , 70 , 71 , 72 , 73 , 74 , 75 , 76 , 77 , 78 .…”

Section: Enhancement Strategies For Tddssmentioning

confidence: 99%

Applications and recent advances in transdermal drug delivery systems for the treatment of rheumatoid arthritis

Zhao

Cao

et al. 2023

Acta Pharmaceutica Sinica B

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Section: Enhancement Strategies For Tddssmentioning

confidence: 99%

Applications and recent advances in transdermal drug delivery systems for the treatment of rheumatoid arthritis

Zhao

Cao

et al. 2023

Acta Pharmaceutica Sinica B

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“…The FT-IR is one of the most important parameters that provide information regarding the interaction of drugs with their excipients. The FT-IR spectra of pure QCT and QCT@NE were obtained using an ATR-FTIR (Bruker OPTIK GmbH Rudolf-Plank-sir.27 D76275, Ettlingen, Germany) instrument in the range of 4000-400 cm −1 [20].…”

Section: Attenuated Total Reflectance-fourier Transform-infra Red (At...mentioning

confidence: 99%

Design-of-Experiments (DoE)-Assisted Fabrication of Quercetin-Loaded Nanoemulgel and Its Evaluation against Human Skin Cancer Cell Lines

et al. 2022

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Background: Quercetin (QCT) is a natural polyphenolic flavonoid showing great potential in the treatment of skin cancer. However, its use is limited owing to its poor water solubility, poor absorption, quick metabolism and excretion, as well as low stability. Preparation of nanoemulgel has been proven to be an effective approach to deliver the drugs topically due to various advantages associated with it. Objectives: This study aimed to prepare stable nanoemulgel of QCT using a Design-of-Experiments (DoE) tool for optimization, to characterize and to assess its in vivo toxicity and efficacy against human cancer cell lines in vitro. Methods: An ultrasonication emulsification method was used for the preparation of QCT-loaded nanoemulsion (QCT@NE). Box–Behnken design was used for the optimization of developed nanoemulgel. Then, in vitro characterization of prepared nanoemulsion was performed using Fourier Transform-Infra Red (FT-IR) spectroscopy, Scanning Electron Microscopy (SEM), particle size analysis, determination of zeta potential and entrapment efficiency (%EE). Further, the developed QCT-loaded nanoemulgel (QCT@NG) was characterized in vitro using texture profile analysis, viscosity and pH determination. Eventually, the cell cytotoxicity studies of the prepared nanoemulgel were performed on the skin cancer cell lines A431 followed by an acute toxicity and skin irritation study on male wistar rats in vivo. Results: The developed QCT@NE was found to be nanometric in size (173.1 ± 1.2 nm) with low polydispersity index (0.353 ± 0.13), zeta potential (−36.1 ± 5.9 mV), and showed good %EE (90.26%). The QCT@NG was found to be substantially more effective against the human skin carcinoma (A431) cell lines as compared to plain QCT with IC50 values of 108.5 and 579.0 µM, respectively. Skin irritation study showed no sign of toxicity and ensured safety for topical application. Hematological analysis revealed no significant differences between the treatment and control group in any biochemical parameter. In the nanoemulgel treatment group, there were no discernible differences in the liver enzymes, bilirubin, hemoglobin, total leukocyte and platelet counts as compared to the control group. Conclusions: The optimized QCT@NG was found to be an ideal and promising formulation for the treatment of skin cancer without showing skin irritation and organ toxicity.

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“…15 Extensive research has been conducted on the use of liposomes in transdermal formulations for various medical conditions, including nutrient deficiencies, transcutaneous immunization, rheumatism, and analgesics. [16][17][18][19] The use of liposomes as a carrier offers several advantages, such as relieving adverse effects, improving bioavailability, controlling drug release, avoiding gastrointestinal problems and first-pass metabolism, and providing greater drug stability. 20 Rodents, particularly rats, have been extensively employed as the animal model in both in vivo and in vitro studies to predict transdermal absorption in human skin during the development of transdermal formulations.…”

Section: Introductionmentioning

confidence: 99%

Preparation of the Levo-Tetrahydropalmatine Liposome Gel and Its Transdermal Study

Zhang¹,

Li²,

Huang³

et al. 2023

IJN

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The aim of this study was to develop a liposome gel containing levo-tetrahydropalmatine (l-THP) and evaluate its transdermal properties. Methods: A L 16 (4 3 ) orthogonal experiment was conducted to optimize the preparation of l-THP liposomes and assess their characterization and stability in a gel. The transdermal features were analyzed through in vivo and in vitro experiments on rats and Strat-M ® membrane, respectively. The metabolism of l-THP in liver and skin S9 fractions was also studied. Results:The optimization of the orthogonal experiment revealed that the ideal mass ratio of phosphatidylcholine, cholesterol, and l-THP during preparation was 10:1:3. The resulting liposome exhibited a particle size of 68 nm, a PDI of 0.27, a drug loading of 4.33%, an encapsulation of 18.79%, and a zeta potential of −41.27 mV. Both the l-THP and its liposome-gel formulation were found to be stable for a duration of 45 days at 4 °C and 30 °C. During the in vivo transdermal study, the maximum concentration (C max ) of l-THP from the liposome gel was 0.16 μg/mL, and the time to reach this maximum concentration (t max ) was 1.2 hours. The relative bioavailability of l-THP in the liposome gel was 233.8% compared to the emulsion. The concentration of l-THP (prepared in PBS) decreased at a rate of 0.0067 μg/mL/min in the liver S9 fraction and 0.0027 μg/mL/min in the skin S9 fraction, however, this difference was not observed when l-THP was encapsulated in liposomes. l-THP passed through the Strat-M ® membrane at a rate of 0.0032 mg/cm 2 /h and 0.002 mg/cm 2 /h for the emulsion and liposome gel, respectively. Conclusion:The optimal process for the preparation of l-THP liposomes was obtained. Compared to the emulsion, the liposomes provided greater bioavailability when used transdermally. The liposomes also provided greater stability for l-THP during storage.

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Liposome and microemulsion loaded with ibuprofen: from preparation to mechanism of drug transport

Cited by 7 publications

References 69 publications

Applications and recent advances in transdermal drug delivery systems for the treatment of rheumatoid arthritis

Applications and recent advances in transdermal drug delivery systems for the treatment of rheumatoid arthritis

Design-of-Experiments (DoE)-Assisted Fabrication of Quercetin-Loaded Nanoemulgel and Its Evaluation against Human Skin Cancer Cell Lines

Preparation of the Levo-Tetrahydropalmatine Liposome Gel and Its Transdermal Study

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