INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2020
·
IF 4.845
Di Zhang,Dan Ye,Panpan Jing,Xiao Tan,Lixia Qiu,Tingting Li,Liyan Shen,Ying Sun,Hongbao Hou,Yunshu Zhang,Qingping Tian
Microemulsion is the preferred vehicle for local anesthetics ; however, the toxicity and irritation associated with a quantity use of surfactants (S) and co-surfactants (CS), i.e., medium- or short-chain alcohols, restrict its commercial application. In this study, efforts have been made to enlarge the CS-free microemulsion area by mixing olive oil (OL) with α-linolenic acid (ALA) and linoleic acid (LA), and by using vitamin E succinate (VES) as an auxiliary oil. Through Box-Behnken design and the optimization of nondominated sorting genetic algorithm II, the optimal microemulsion formulation (M E0 ) with a large steady-state simultaneous permeation rate ( J s ) and skin retention was screened as 3.23% OL, 0.45% ALA , 1.81% LA, 0.91% VES, 13.60% S, 5% lidocaine and water. Three percent ethanol was screened as a permeability enhancer for the hydrogel of M E0 , which showed a statistical increase in J s and skin retention through the abdominal skin of guinea pigs. The optimized formulation had desirable characterization, good stability and negligible irritation. The large J s and skin retention were well reflected in the pinprick test, wherein intensity of anesthetic effect and duration of action were increased significantly over the commercial cream. The developed CS-free microemulsion hydrogel with low S could be a promising strategy for the topical delivery of lidocaine.
研究领域:
药剂学
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药物递送系统
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产品关联
DOI
PubMed
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
·
2017
·
IF 3.887
Yibang Zhang,Weibeng Ng,Jianguo Hu,Salma Saleh Mussa,Yanru Ge,Huaxi Xu
The primary objective of this study was to develop, evaluate and compare the effectiveness and stability of ethosomal carbomer gels in different solvents. The optimal ethosomal formulation was isolated to create ethosomal gels using carbomer in either pure water (water gel) or PBS containing 30% ethanol (PBS gel). In vitro release of the ethosomal gels were tested using Franz apparatus on hydrophilic and hydrophobic artificial membranes. In vitro stability of two ethosomal gels was systematically evaluated. Transdermal antigen delivery of ethosomal gel was finally performed on the skin of hair removal mice. Both solvent and concentration effects on the in vitro release performance of ethosomal gel of carbomer have been confirmed. Penetration depth has been found to be dependent on the nature of the membranes such that penetration rate is higher in the hydrophobic membrane than the hydrophilic ones. Furthermore, in vitro stability test indicated that ethosomal PBS gel was more stable than ethosomal water gel. In vivo immunoassay confirmed that the ethosomal PBS gel could deliver the antigenic molecules into the skin of mice and stimulate specific IgG secretion. Using the same solvent for lipid vesicular formulation when making polymeric hydrogel may help to provide a more conducive environment for lipid vesicles and hence enhance their roles in transdermal antigen delivery.
研究领域:
药剂学
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免疫学
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2022
·
IF 6.51
Xier Pan,Yushu Li,Weilin Pang,Yaqi Xue,Zhuxian Wang,Cuiping Jiang,Chunyan Shen,Qiang Liu,Li Liu
Poly(vinyl alcohol) (PVA) and carbomer were used as the hydrogel system to fabricate glabridin-loaded hydrogel-forming microneedles (HFMNs) by chemical cross-linking (CCMNs) and physical cross-linking (PCMNs). The properties and drug permeation effects of glabridin-loaded HFMNs with different methods were compared. They both owned excellent shapes, mechanical and insertion properties. PCMNs showed collapsed shapes during swelling due to the low cross-linking rate and high porosity, which probably results in resealing of skin pores during transdermal drug delivery. However, CCMNs could rapidly swell within 2 h with slightly bending. The infrared spectra indicate that CCMNs and PCMNs might form the hydrogel network by generating hydrogen and covalent bonds, respectively. The in vitro release studies showed that cumulative permeation amount within 24 h (1654 μg/cm 2 ) of CCMNs significantly higher than that (372 μg/cm 2 ) achieved by PCMNs and that (118 μg/cm 2 ) achieved by glabridin-loaded gel. The skin barrier recovery test suggests the desirable security of both microneedles (MNs), notwithstanding the presence of mild erythema in the mouse skin applied CCMNs. These results indicate that CCMNs were more desirable for glabridin delivery using PVA and carbomer as a skeleton of the hydrogel network.
研究领域:
药剂学
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生物材料
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皮肤科学
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产品关联
DOI
PubMed
高影响因子
Revista Brasileira de Farmacognosia-Brazilian Journal of Pharmacognosy
·
2023
·
IF 1.6
Su Jiangtao,Zhang Yuxuan,Ye Lu,Chen Xue,Hu Yuchen
Psoriasis is a chronic papulosquamous skin disease whose current treatments have severe side effects, which limits their long-term application. Developing effective treatments for psoriasis is an important and challenging task. Coptis chinensis Franch., Ranunculaceae, and Phellodendron amurense Rupr., Rutaceae, are widely used in traditional Chinese medicine to treat psoriasis. Therefore, this article aims to construct a thermo-sensitive local administration system based on multiple alkaloids from C. chinensis and P. amurense . The methods of extracting the effective components of C. chinensis and P. amurense were screened by single-factor experiment and orthogonal experiment. Furthermore, the optimal gel formulation was determined, and the obtained CPG-S hydrogel ( C. chinensis and P. amurense gel with S -nitrosated acetylpenicillamine as a penetration promoter) exhibited thermo-sensitivity and excellent transdermal ability. Then, the therapeutic effect of the CPG-S hydrogel was examined in a psoriasis mouse model. The effectiveness of the CPG-S hydrogel in reducing the symptoms of redness, swelling, and squamous epidermis, as well as downregulating the related inflammatory factors IL-17A and IL-23, was confirmed. The CPG-S hydrogel was found to be more effective than the commercially available psoriasis treatment drug mometasone furoate cream, indicating its potential application as an effective psoriasis treatment drug. Graphical abstract
研究领域:
药剂学
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中医药学
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皮肤病学
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产品关联
DOI
高影响因子
Materials Science & Engineering C-Materials for Biological Applications
·
2018
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IF 5.08
Depeng Liu,Bo Yu,Guohua Jiang,Weijiang Yu,Yang Zhang,Bin Xu
Dissolving microneedles (MNs) display high efficiency, safety and painless in transdermal delivery for poorly permeable drugs. Here, a dissolving composite MNs prepared from insulin-loaded CaCO 3 microparticles (INS-CaCO 3 MPs) and poly(vinyl pyrrolidone) (PVP) as matrix were fabricated with two-step centrifuging and molding process to immobilize insulin in the MNs. The as-prepared INS-CaCO 3 /PVP MNs exhibited remarkable mechanical strength and slower solubility properties when compared with pure PVP MNs. In vitro skin insertion capability was determined by staining with FITC-labeled insulin which was revealed after insertion, gradually diffusing from the puncture sites to deeper tissues. In vivo pharmacodynamic studies were then conducted to estimate the feasibility of the administration of insulin-loaded dissolving MNs on diabetic rats for glucose regulation. The relative pharmacological availability ( RPA ) and relative bioavailability ( RBA ) of insulin from MNs were 98.2 and 96.6%. Thus, this study suggests that the use of INS-CaCO 3 /PVP MNs achieved both high efficiency and constant release of insulin in comparison with the traditional subcutaneous injection approach and presented a promising device to delivery insulin for diabetic therapy.
研究领域:
药剂学
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糖尿病治疗
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生物材料科学
✓ 已验证
DOI
PubMed
高影响因子
LANGMUIR
·
2025
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IF 3.9
Nipeng Chen,Zhipeng Zeng,Haolin Chen,Hong Liu,Zhihui Zhang,Fangfang Ke,Xiaoyu Ji,Lixin Liu,Zhen Zhang,Yongming Chen
Liraglutide, a glucagon-like peptide-1 (GLP-1) receptor agonist, is recognized for its effectiveness in glycemic control and weight reduction. However, the pain associated with the traditional subcutaneous administration of liraglutide and needle phobia in some patients will seriously affect medication adherence. Transdermal delivery represents a promising alternative to subcutaneous injection for its convenience, noninvasiveness, and painlessness, and it can bypass the first-pass metabolism and multiple biological barriers of oral administration and be delivered in a controlled manner, resulting in steady drug levels. Nonetheless, due to skin barriers, effective transdermal delivery of peptide-based drugs like liraglutide remains challenging. This study developed a two-step platform for preparing peptide nanoparticles based on flash nanocomplexation (FNC) technology to improve the efficacy of transdermal liraglutide delivery. Liraglutide was first encapsulated in nanoparticles formed by tannic acid (TA) and aluminum ions (Al3+), wherein coordination interactions between TA and Al3+, as well as hydrogen bonding interactions involving TA and liraglutide. Then, liraglutide nanoparticles were coated with positively charged hydroxypropyl trimethylammonium chloride chitosan (HTCC) to improve transdermal delivery efficacy. The resulting liraglutide nanoparticles exhibited superior transdermal penetration, durable hypoglycemic effects, and long-acting therapeutic efficacy for obesity, indicating that the developed Lira nanoparticle offers a promising platform for the transdermal delivery of peptide-based drugs.
研究领域:
药剂学
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生物医学工程
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代谢疾病研究
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DOI
PubMed
高影响因子
AAPS PHARMSCITECH
·
2025
·Vol. 26
·期 1
·1-17
·
IF 4
Gu Qifei,Xiao Wuqing,Zhu Yingyin,Zhong Wanling,Sui Xue,Liu Yongchao,Zhang Jie,Wu Huichao,Zhou Rui
Paeoniflorin is a natural pharmaceutical ingredient with a widely biological activity. However, as a hydrophilic drug, the problem of low transdermal rate limits its clinical application. To overcome this shortage, LUVs were used as biocompatible carriers of paeoniflorin in this study. We prepared paeoniflorin-loaded large unilamellar vesicles (LUVs) with W/O/W structure by microfluidics. We used four kinds of chips to prepare paeoniflorin LUVs and explored the effects of the chip structures on LUVs properties applying both experiments and numerical simulations. The difference of fluid mixing mechanisms was analyzed among four different channels, including straight and curved structures. Then we evaluated the differences in skin permeability among the three groups, paeoniflorin aqueous solution group, drug-loaded liposome group and blank liposome & drug mixture group, using the abdominal skin of male mice. The results showed that the structure of the microfluidic channel was a key factor affecting the flow rate and mixing efficiency. The mixing efficiency further affected the liposome size. The mixing efficiency of curved channel was not better than that of a straight channel due to the low flow rate and long mixing time. By the results of transdermal experiments, LUVs could reduce the transdermal time and increase the total transdermal amount. LUVs effectively improved the transdermal absorption efficiency of paeoniflorin. In conclusion, paeoniflorin LUVs with highly efficient transdermal were successfully prepared by using microfluidics. We explored the underlying fluid dynamics that lead to variations in the preparation with different chip structures. The transdermal effect of the LUVs was verified. Graphical
研究领域:
药剂学
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生物医学工程
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产品关联
DOI
PubMed
高影响因子
International Journal of Polymeric Materials and Polymeric Biomaterials
·
2019
·
IF 2.263
Yang Zhang,Dongning Chai,Mengyue Gao,Bin Xu,Guohua Jiang
The separable microneedles (MNs), consisted of upper metformin-loaded PCL arrowheads and lower PVA/PCL supporting array, have been fabricated by separately molding method. The metformin-loaded and thermal ablation MNs arrowheads were capped on dissolving solid supporting array. The as-fabricated MNs exhibited an excellent thermal ablation change due to the low melting point of PCL. After insertion into the skin, the upper separable MNs arrowheads could be embedded into the skin. When the separable MNs arrowheads were exposed to thermal stimulus, causing the PCL MNs arrowheads to melt and enabling the release of encapsulated metformin to be thermally modulated.
研究领域:
药剂学
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生物医学工程
·
糖尿病研究
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产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2020
·
IF 5.162
Xiying Wu,Hongmin Zhang,Shuhua He,Qin Yu,Yi Lu,Wei Wu,Ning Ding,Quangang Zhu,Zhongjian Chen,Yuhua Ma,Jianping Qi
The aim of this study is to evaluate the enhanced ability of various choline based ionic liquids (ILs) for dermal delivery of hyaluronic acid (HA). Eight ILs were synthesized via neutralization reactions, which were characterized using Fourier transform infrared spectrometer and proton nuclear magnetic resonance. The enhanced capacity of ILs varied with organic acids. The IL formed by choline and citric acid ([Ch][Cit]) exerted the strongest ability to promote HA penetrating deep into the skin among all ILs. The enhanced ability of [Ch][Cit] were still maintained and even improved after diluted by water although it could be disassociated partially according to electricity. The moisture and transepidermal water loss (TEWL) were employed to evaluate the effect of attenuating skin dehydration. As expected, the IL of choline and malic acid ([Ch][Mala]) and [Ch][Cit] increased moisture and decreased TEWL significantly by improving the penetration of HA into skin. Meanwhile, no irritation was observed on skin of nude mice after treatment by the three ILs which showed optimal enhanced effect. In conclusion, ILs could be high potential biocompatible carriers for facilitating HA dermal delivery to resist skin dehydration for medical or cosmetic uses.
研究领域:
药剂学
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化妆品学
·
化学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2022
·
IF 5.062
Lijuan Ye,Weibin Chen,Yuan Chen,Yuqin Qiu,Jun Yi,Xiaofang Li,Qiuxiao Lin,Bohong Guo
Transdermal administration is a promising non-invasive and convenient method of drug delivery in clinic and avoid serious gastrointestinal adverse reactions. In this study, a hybrid nanocarrier was developed to facilitate transdermal delivery of drugs. The low water-soluble ketoprofen (KP) was ultrasonically loaded on functionalized multi-walled carbon nanotubes (f-MWCNTs), and the preparation process was optimized using Box-Behnken design. Then, KP-loaded f-MWCNTs composite ethosomes (f-MWCNTs-KP-ES) were prepared by a single-step injection technology. Over the study period, the preparation was verified by a series of characterizations, and ex vivo release characteristics, ex vivo permeation of rat skin and in vivo pharmacokinetics were studied. The characterization results consistently showed that f-MWCNTs-KP-ES were successfully prepared. The preparation can obviously improve the solubility of KP. Ex vivo permeation experiments showed that had a sustained release effect and the skin penetration rate of f-MWCNTs-KP-ES gel is the fastest, with a cumulative permeation amount of 602.35 ± 41.06 μg/cm 2 . In addition, both ethosomes and f-MWCNTs could increase the retention of drugs and form drug reservoirs. Fluorescence microscope images of rat skin clearly illustrated the faster and deeper penetration of f-MWCNTs composite ethosomes formulation loaded with rhodamine B (RB) (f-MWCNT-RB-ES). In vivo pharmacokinetic experiments showed the area under the drug time curve (AUC 0-t ) and elimination half-life (T 1/2β ) of f-MWCNTs-KP-ES gel group were significantly increased and prolonged compared with KP commercial gel group, respectively. The overall data indicate that the f-MWCNTs composite ethosomes formulation is a promising transdermal drug delivery system .
研究领域:
药剂学
·
生物医学工程
·
药物递送系统
✓ 已验证
产品关联
DOI
高影响因子
PHARMAZIE
·
2023
·Vol. 78
·期 5
·31-36
·
IF 1.6
Xiaowei J.,Lijuan Y.,Yanling L.,Qiuxiao L.,Bohong G.
The purpose of this study was to combine carbon nanotube with ethosomes in order to obtain hybrid nanocarriers for transdermal delivery of ketoprofen (KP). KP-loaded functionalized single-walled carbon nanotube (f-SWCNTs) composite ethosomes (f-SWCNTs-KP-ES) were designed and were verified
by a series of characterizations. The particle size of the preparation is less than 400 nm. DSC and XRD experiments showed that KP existed in an amorphous state after it was adsorbed and loaded on f-SWCNTs. TEM experiments showed that the structure of SWCNTs remained intact after oxidation
and modification by PEI. FTIR results showed that PEI were successfully modified on the surface of SWCNT-COOH, and KP was successfully loaded on f-SWCNTs. In vitro release characteristics showed that the preparation had sustained release behavior and conformed to the first-order kinetic
equation model. In addition, f-SWCNTs-KP-ES gel were prepared and in vitro skin permeation and in vivo pharmacokinetics were studied. The results showed that f-SWCNTs-KP-ES gel could enhance the skin permeation rate of KP and increase the drug retention of drugs in the skin.
The characterization results consistently showed f-SWCNTs is a promising drug carrier. The hybrid nanocarrier prepared by the combination of f-SWCNTs and ethosomes can enhance the transdermal absorption of drugs and improve the bioavailability of drugs, which has a certain significance for
the development of advanced hybrid nano-preparations.
研究领域:
药剂学
·
纳米医学
·
药物递送系统
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产品关联
DOI
PubMed
高影响因子
ACS Applied Bio Materials
·
2018
·
IF 0
Hui-Jiuan Chen,Di-an Lin,Fanmao Liu,Lingfei Zhou,Di Liu,Zhihong Lin,Chengduan Yang,Quanchang Jin,Tian Hang,Gen He,Xi Xie
Bioactive functional probiotics play an important role in many health applications such as maintaining skin health and the immunity of the human host. Artificial supplementation of probiotics would enhance immune functions as well as regulate skin health. However, simple and effective methods to deliver probiotics into the dermis to regulate local dermal tissue are still lacking. Furthermore, microneedles have been used for transdermal drug delivery in a pain-free manner, yet there were few reported methods to deliver living microbes via microneedles. In this work, we developed a technique to deliver bioactive functional probiotics, using lactobacillus as the model probiotic, into local dermis by dissolvable microneedles. The transdermal delivery of probiotics might enhance local skin regulation and immunity, and dissolvable microneedles served as a safe and pain-free tool for dermal microbial delivery. Lactobacillus was encapsulated in dissolvable microneedles with high viability by a centrifugation casting method. The microneedles rapidly dissolved after skin penetration, releasing the lactobacillus into the subcutaneous space, without causing local tissue irritation. The lactobacillus was functionally bioactive following transdermal delivery, actively synthesizing lactic acid both ex vivo and in vivo. Our technique provided a safe, effective, and convenient approach for the transdermal delivery of probiotics into local skin, with the potential to improve skin health and immunity.
研究领域:
生物医学工程
·
微生物学
·
药剂学
✓ 已验证
DOI
PubMed
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