Improving Topical Skin Delivery of Monocrotaline Via Liposome Gel-based Nanosystems

2019 ◽  
Vol 16 (10) ◽  
pp. 940-950 ◽  
Author(s):  
Jiandong Yu ◽  
Zhi Chen ◽  
Yan-zhi Yin ◽  
Chaoyuan Tang ◽  
Enying Hu ◽  
...  
Keyword(s):  
Gradient Method ◽  
Encapsulation Efficiency ◽  
Ph Value ◽  
Topical Administration ◽  
Ph Gradient ◽  
Stability Factor ◽  
Buffer Solution ◽  
Skin Delivery ◽  
Skin Retention

Background: In this study, a liposomal gel based on a pH-gradient method was used to increase the skin-layer retention of monocrotaline (MCT) for topical administration. Methods: Using the Box-Behnken design, different formulations were designed to form liposome suspensions with optimal encapsulation efficiency (EE%) and stability factor (KE). In order to keep MCT in liposomes and accumulate in skin slowly and selectively, MCT liposome suspensions were engineered into gels. Results: A pH-gradient method was used to prepare liposome suspensions. The optimal formulation of liposome suspensions (encapsulation efficiency: 83.10 ± 0.21%) was as follows: MCT 12 mg, soybean phosphatidyl choline (sbPC) 200 mg, cholesterol (CH) 41 mg, vitamin E (VE) 5 mg, and citric acid buffer solution (CBS) 4.0 10 mL (pH 7.0). The final formulation of liposomal gels consisted of 32 mL liposome suspensions, 4.76 mL deionized water, 0.40 g Carbopol-940, 1.6 g glycerol, 0.04 g methylparaben, and a suitable amount of triethanolamine for pH value adjustment. The results of in vitro drug release showed that MCT in liposomal gels could be released in 12 h constantly in physiological saline as a Ritger-Peppas model. Compared with plain MCT in gel form, liposomal MCT in gel had higher skin retention in vitro. Conclusion: In this study, liposomal gels were formed for greater skin retention of MCT. It is potentially beneficial for reducing toxicities of MCT by topical administration with liposomal gel.

scholarly journals An Investigation of the Influence of PEG 400 and PEG-6-Caprylic/Capric Glycerides on Dermal Delivery of Niacinamide

Polymers ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 2907
Author(s):  
Yanling Zhang ◽  
Majella E. Lane ◽  
David J. Moore
Keyword(s):  
Skin Permeation ◽  
Ternary Systems ◽  
Pharmaceutical Products ◽  
Porcine Skin ◽  
Peg 400 ◽  
Skin Delivery ◽  
Dermal Delivery ◽  
Binary And Ternary Systems ◽  
Skin Retention

Polyethylene glycols (PEGs) and PEG derivatives are used in a range of cosmetic and pharmaceutical products. However, few studies have investigated the influence of PEGs and their related derivatives on skin permeation, especially when combined with other solvents. Previously, we reported niacinamide (NIA) skin permeation from a range of neat solvents including propylene glycol (PG), Transcutol® P (TC), dimethyl isosorbide (DMI), PEG 400 and PEG 600. In the present work, binary and ternary systems composed of PEGs or PEG derivatives combined with other solvents were investigated for skin delivery of NIA. In vitro finite dose studies were conducted (5 μL/cm2) in porcine skin over 24 h. Higher skin permeation of NIA was observed for all vehicles compared to PEG 400. However, overall permeation for the binary and ternary systems was comparatively low compared with results for PG, TC and DMI. Interestingly, values for percentage skin retention of NIA for PEG 400:DMI and PEG 400:TC were significantly higher than values for DMI, TC and PG (p < 0.05). The findings suggest that PEG 400 may be a useful component of formulations for the delivery of actives to the skin rather than through the skin. Future studies will expand the range of vehicles investigated and also look at skin absorption and residence time of PEG 400 compared to other solvents.

In Vitro Dissolution Behavior of Biphasic Tricalcium Phosphate Composite Powders Composed of α-Tricalcium Phosphate and β-Tricalcium Phosphate

2008 ◽  
Vol 368-372 ◽  
pp. 1206-1208 ◽  
Author(s):  
Yan Bao Li ◽  
Dong Xu Li ◽  
Wen Jian Weng
Keyword(s):  
Heat Treatment ◽  
Calcium Phosphate ◽  
Tricalcium Phosphate ◽  
Amorphous Calcium Phosphate ◽  
Ph Value ◽  
In Vitro Dissolution ◽  
Dissolution Behavior ◽  
Buffer Solution ◽  
Composite Powders

Biphasic tricalcium phosphate (BTCP) powders composed of α-tricalcium phosphate (α-TCP) and β-tricalcium phosphate (β-TCP) were prepared using amorphous calcium phosphate (ACP) precursor after heat treatment at 800oC. The in vitro dissolution behavior of the powders was examined after soaked in 0.1M NaAc-HAc buffer solution for different times. It was revealed that the Ca2+ and PO4 3- concentration, and pH value of the BTCP-soaked solution are higher than those of the α-TCP- and β-TCP-soaked solutions. The dissolution behavior of BTCP powders was explained. The specific dissolution behavior of BTCP powders can widen the biodegradation range of calcium phosphate family.

Nanoliposomes@Transcutol for In Vitro Skin Delivery of 8-Methoxypsoralen

2021 ◽  
Vol 21 (5) ◽  
pp. 2901-2906
Author(s):  
Chiara Sinico ◽  
Anna Maria Fadda ◽  
Donatella Valenti ◽  
Rosa Pireddu ◽  
Francesco Corrias ◽  
...  
Keyword(s):  
Oral Administration ◽  
Encapsulation Efficiency ◽  
Human Keratinocytes ◽  
Penetration Enhancer ◽  
Skin Permeability ◽  
Skin Delivery ◽  
Skin Accumulation ◽  
Significant Difference ◽  
Franz Diffusion Cells

8-methoxypsoralen is the most common drug in psoralen plus ultraviolet light irradiation therapy for the treatment of severe psoriasis. Despite of the efficacy, its classic oral administration leads to several serious adverse effects. However, the topical psoralen application produces a drug skin accumulation lower than that obtained by oral administration, due to the drug low skin permeability. In this paper, 8-methoxypsoralen loaded Penetration Enhancer-containing Vesicles were prepared using soy phosphatidylcholine and the penetration enhancer Transcutol® (5% or 10%) and characterized in terms of size, polydispersity index, zeta potential and encapsulation efficiency. No statistically significant differences in both size (~135 nm) and encapsulation efficiency (~65%) were found for different Transcutol® concentration. Transdermal delivery study assessed by Franz diffusion cells, showed that the 8-methoxypsoralen mainly accumulated into the stratum corneum. Moreover, after Penetration Enhancer-containing Vesicles application, the drug recovered in this layer is almost double of that delivered by conventional liposomes, while no significant difference was found from the different Transcutol® concentrations. Finally, biocompatibility checked by an MTT assay, demonstrated that the incubation of human keratinocytes for 24 h with 8-methoxypsoralen loaded Penetration Enhancer-containing Vesicles did not significantly reduce cell viability.

scholarly journals The Degradation Properties of MgO Whiskers/PLLA Composite In Vitro

2018 ◽  
Vol 19 (9) ◽  
pp. 2740 ◽  
Author(s):  
Yun Zhao ◽  
Bei Liu ◽  
Hongwei Bi ◽  
Jinjun Yang ◽  
Wei Li ◽  
...  
Keyword(s):  
Ph Value ◽  
Composite Films ◽  
Phosphate Buffer Solution ◽  
Buffer Solution ◽  
In Vitro Degradation ◽  
Final Weight ◽  
Cell Affinity ◽  
Degradation Properties ◽  
Composite Samples

In this study, composite films of stearic acid–modified magnesium oxide whiskers (Sa–w-MgO)/poly-l-lactic acid (PLLA) were prepared through solution casting, and the in vitro degradation properties and cytocompatibility of the composites with different whisker contents were investigated. The results showed that the degradation behavior of the composite samples depended significantly on the whisker content, and the degradation rate increased with the addition of MgO content. Furthermore, the degradation of the composites with higher contents of whiskers was influenced more severely by the hydrophilicity and pH value, leading to more final weight loss, but the decomposition rate decreased gradually. Furthermore, the pH value of the phosphate buffer solution (PBS) was obviously regulated by the dissolution of MgO whiskers through neutralization of the acidic product of PLLA degradation. The cytocompatibility of the composites also increased remarkably, as determined from the cell viability results, and was higher than that of PLLA at the chosen whisker content. This was beneficial for the cell affinity of the material, as it notably led to an enhanced biocompatibility of the PLLA, in favor of promoting cell proliferation, which significantly improved its bioactivity, as well.

scholarly journals Effects of Magnesium Oxide (MgO) Shapes on In Vitro and In Vivo Degradation Behaviors of PLA/MgO Composites in Long Term

Polymers ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 1074 ◽  
Author(s):  
Yun Zhao ◽  
Hui Liang ◽  
Shiqiang Zhang ◽  
Shengwei Qu ◽  
Yue Jiang ◽  
...  
Keyword(s):  
Magnesium Oxide ◽  
Ph Value ◽  
Phosphate Buffer Solution ◽  
Buffer Solution ◽  
Biomedical Material ◽  
Degradation Behaviors ◽  
In Vivo Degradation

Biodegradable devices for medical applications should be with an appropriate degradation rate for satisfying the various requirements of bone healing. In this study, composite materials of polylactic acid (PLA)/stearic acid-modified magnesium oxide (MgO) with a 1 wt% were prepared through blending extrusion, and the effects of the MgO shapes on the composites’ properties in in vitro and in vivo degradation were investigated. The results showed that the long-term degradation behaviors of the composite samples depended significantly on the filler shape. The degradation of the composites is accelerated by the increase in the water uptake rate of the PLA matrix and the composite containing the MgO nanoparticles was influenced more severely by the enhanced hydrophilicity. Furthermore, the pH value of the phosphate buffer solution (PBS) was obviously regulated by the dissolution of MgO through the neutralization of the acidic product of the PLA degradation. In addition, the improvement of the in vivo degrading process of the composite illustrated that the PLA/MgO materials can effectively regulate the degradation of the PLA matrix as well as raise its bioactivity, indicating the composites for utilization as a biomedical material matching the different requirements for bone-related repair.

The Release Characteristics of Different Model Drugs from Medicated PLGA Microspheres

2014 ◽  
Vol 936 ◽  
pp. 746-750 ◽  
Author(s):  
Tong Chen ◽  
Yuan Yuan Liang ◽  
Ying Ge Zhao ◽  
Xiao Yun Zhang ◽  
Tong Sheng Qi ◽  
...  
Keyword(s):  
Encapsulation Efficiency ◽  
Water Solubility ◽  
Phosphate Buffer Solution ◽  
Plga Microspheres ◽  
Release Rates ◽  
Buffer Solution ◽  
Surface Morphologies ◽  
Scanning Electron ◽  
Release Profiles

In this study, four model drugs, i.e., Meloxicam (MEL), Risperidone (RIS), Eprinomectin (EPR), and Bull Serum Albumin (BSA), were encapsulated in PLGA microspheres via solvent evaporation methods. The encapsulation efficiency and in vitro release profiles of different drugs with various water solubilities from medicated PLGA microspheres were investigated. The surface morphologies of microspheres were detected by scanning electron microscope (SEM). The release characteristics of the model drugs from the medicated microspheres were carried out in the phosphate buffer solution (PBS), pH7.4, at 37 °C. Studies found that the water solubility of model drugs had significant influences on their in vitro release profiles and the release rates of four model drugs were in the orders of BSA＞MEL＞RIS＞EPR.

Designing a novel in vitro drug-release-testing method for liposomes prepared by pH-gradient method

2012 ◽  
Vol 430 (1-2) ◽  
pp. 381-387 ◽  
Author(s):  
Koji Nakamura ◽  
Keisuke Yoshino ◽  
Keiko Yamashita ◽  
Hiroaki Kasukawa
Keyword(s):  
Drug Release ◽  
Gradient Method ◽  
Ph Gradient ◽  
In Vitro Drug Release ◽  
Testing Method ◽  
Release Testing

scholarly journals In Vitro Structural Changes of Nano-Bacterial Cellulose Immersed in Phosphate Buffer Solution

2011 ◽  
Vol 10 ◽  
pp. 55-66 ◽  
Author(s):  
Yan Mei Chen ◽  
Ting Fei Xi ◽  
Yu Feng Zheng ◽  
Liang Zhou ◽  
Yi Zao Wan
Keyword(s):  
Bacterial Cellulose ◽  
Phosphate Buffer ◽  
Structural Changes ◽  
Ph Value ◽  
Phosphate Buffer Solution ◽  
Buffer Solution ◽  
Potential Applications ◽  
Scaffold Materials

Nano-bacterial cellulose (nBC), secreted by Acetobacter xylinum, is expected to have potential applications in tissue engineering. In this paper, the in-vitro degradation performance and the corresponding mechanism of nBC immersed in phosphate buffer solution (PBS) for different time periods was investigated. The pH value variation of solution, material degradation, and the swelling and structural changes of nBC was analysed successively. The results indicate that water molecules attack the exposed nBC fibrils, weakening the bonding strength of inter- and intra-molecular chains and disconnecting partial C-O-C bonds. The disconnection of C-O-C bonds is considered the primary reason for the degradation of nBC large molecular chains after nBC is immersed in PBS. The present work is instructive for controlling the in-vivo degradation performance of nBC acting as bone tissue engineered scaffold materials.

scholarly journals Niosomal Nanocarriers for Enhanced Skin Delivery of Quercetin with Functions of Anti-Tyrosinase and Antioxidant

Molecules ◽  
2019 ◽  
Vol 24 (12) ◽  
pp. 2322 ◽  
Author(s):  
Banyi Lu ◽  
Yanting Huang ◽  
Zhongyun Chen ◽  
Jingyi Ye ◽  
Hongyu Xu ◽  
...  
Keyword(s):  
Zeta Potential ◽  
Ex Vivo ◽  
Radical Scavenging ◽  
Entrapment Efficiency ◽  
Potential Range ◽  
Skin Delivery ◽  
Antioxidant Capacities ◽  
Drug Entrapment Efficiency ◽  
Skin Retention

This study aimed to screen an effective flavonoid with promising whitening and antioxidant capacities, and design flavonoid-loaded niosomes to improve its solubility, stability, and penetration. In vitro anti-tyrosinase and 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging experiments were conducted to investigate the whitening and antioxidant capacities of several flavonoids, including quercetin, morin, festin, myricetin, rutin, and breviscapine. The conductivity, viscosity, and particle size of Span60-RH40-based formulation of nonionic surfactant vesicles (niosomes) with different mass ratios were studied to determine the most appropriate formulation. Drug-loaded niosomes were characterized for size, zeta potential, morphology, and entrapment efficiency. The photostability, solubility, release behavior, ex vivo drug penetration, and skin retention were also studied. The results showed that quercetin has considerable whitening and antioxidant capacities and Span60-RH40 at a mass ratio of 9:11 forms spherical or oval niosomes of 97.6 ± 3.1 nm with a zeta potential range of 31.1 ± 0.9 mV, and drug entrapment efficiency as high as 87.3 ± 1.6%. Niosomes remarkably improved the solubility and photostability of quercetin. Furthermore, compared to quercetin solution, quercetin-niosomes had the advantages of sustained release and improved transdermal penetration, with skin retention 2.95 times higher than quercetin solution.

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