APPLIED SURFACE SCIENCE
·
2011
·
IF 1.795
Qinfu Zhao,Tianyi Wang,Jing Wang,Li Zheng,Tongying Jiang,Gang Cheng,Siling Wang
In order to improve the dissolution rate and increase the bioavailability of a poorly water-soluble drug, intended to be administered orally, the biocompatible and bioactive mesoporous hydroxyapatite (HA) was successfully synthesized. In the present study, mesoporous HA nanoparticles were produced using Pluronic block co-polymer F127 and cetyltrimethylammonium bromide (CTAB) as templates by the hydrothermal method. The obtained mesoporous HA was employed as a drug delivery carrier to investigate the drug storage/release properties using carvedilol (CAR) as a model drug. Characterizations of the raw CAR powder, mesoporous HA and CAR-loaded HA were carried out by the scanning electron microscopy (SEM), transmission electron microscopy (TEM), X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), Fourier transform infrared (FT-IR) spectroscopy, N 2 adsorption/desorption, thermogravimetric analysis (TGA), and UV–VIS spectrophotometry. The results demonstrated that CAR was successfully incorporated into the mesoporous HA host. In vitro drug release studies showed that mesoporous HA had a high drug load efficiency and provided immediate release of CAR compared with micronized raw drug in simulated gastric fluid (pH 1.2) and intestinal fluid (pH 6.8). Consequently, mesoporous HA is a good candidate as a drug carrier for the oral delivery of poorly water-soluble drugs.
研究领域:
药剂学
·
生物材料
·
药物传递
·
纳米医学
·
药代动力学
✓ 已验证
DOI
高影响因子
MOLECULAR PHARMACEUTICS
·
2015
·
IF 4.384
Jianbin Zhang,Yan Lv,Bing Wang,Shan Zhao,Mingqian Tan,Guojun Lv,Xiaojun Ma
Mucus layer, a selective diffusion barrier, has an important effect on the fate of drug delivery systems in the gastrointestinal tract. To study the fate of microemulsions in the mucus layer, four microemulsion formulations with different particle sizes and lipid compositions were prepared. The microemulsion–mucin interaction was demonstrated by the fluorescence resonance energy transfer (FRET) method. Moreover, the microemulsions were observed aggregated into micron-sized emulsions by laser confocal microscopy. We concluded the microemulsion–mucin interaction not only led to microemulsions closely adhered to mucins but also destroyed the structure of microemulsions. At last, the diffusion of blank microemulsions and microemulsion-carried drugs (resveratrol and hymecromone) through mucin solutions was determined by the fluorescence recovery after photobleaching (FRAP) method and the Franz diffusion cell method. The results demonstrated the diffusion of microemulsions was significantly hindered by mucin solutions. The particle size of microemulsions had a negligible effect on the diffusion coefficients. However, the type of lipid played an important role, which could form hydrophobic interactions with mucins. Interestingly, microemulsion-carried drugs with different core/shell locations seemed to suffer different fates in the mucin solutions. The drug incorporated in the oil core of microemulsions, resveratrol, was transported through the mucus layer by the carriers, while the drug incorporated in the surfactant shell of microemulsions, hymecromone, was separated from the carriers and diffused toward the epithelium in the form of free molecules.
研究领域:
药剂学
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
CRYSTAL GROWTH & DESIGN
·
2016
·
IF 4.425
Xia-Lin Dai,Song Li,Jia-Mei Chen,Tong-Bu Lu
Pharmaceutical cocrystallization is proposed as a new method to enhance membrane permeability of a BCS class III model drug, 5-fluorouracil (5FU). Three cocrystals of 5FU, 5FU/3-hydroxybenzoic acid (1), 5FU/4-aminobenzoic acid (2), and 5FU/cinnamic acid (3), were successfully synthesized by a slurry method or a liquid-assisted grinding process. Spectroscopic methods, thermal analysis, and X-ray diffraction were used to characterize these new forms. The permeability was studied using a Franz diffusion cell and silicone membrane. All of the cocrystals showed improved membrane permeability compared to free 5FU. The cumulative amount per unit area of permeated 5FU in the first 10 h for 1–3 was increased by 41, 70, and 83%, and the steady penetration rates of 1–3 were increased by 38, 66, and 79%, respectively, as compared to the pure drug. Structure–permeability correlation study finds a link between intermolecular interactions and molecular packing in cocrystals and their permeability behavior and has important implications for use of a cocrystallization approach to improve drugs’ permeability in the pharmaceutical field.
研究领域:
药学
·
生物医学工程
·
药物化学
✓ 已验证
DOI
高影响因子
Nanoscale
·
2014
·Vol. 6
·期 11
·6141-6150
·
IF 6.739
Xinchao Yang,Nana Zhao,Fu-Jian Xu
Graphene oxide (GO) has been proven to be promising in many biomedical fields due to its biocompatibility, unique conjugated structure, easily tunable surface functionalization and facile synthesis. In this work, a flexible two-step method was first developed to introduce the atom transfer radical polymerization (ATRP) initiation sites containing disulfide bonds onto GO surfaces. Surface-initiated ATRP of (2-dimethyl amino)ethyl methacrylate (DMAEMA) was then employed to tailor the GO surfaces in a well-controlled manner, producing a series of organic–inorganic hybrids (termed as SS–GPDs) for highly efficient gene delivery. Under reducible conditions, the PDMAEMA side chains can be readily cleavable from the GO backbones, benefiting the resultant gene delivery process. Moreover, due to the conjugated structure of the graphene basal plane, SS–GPD can attach and absorb aromatic, water insoluble drugs, such as 10-hydroxycamptothecin (CPT), producing SS–GPD–CPT. The MTT assay and the simultaneous double-staining procedure revealed that SS–GPD–CPT possessed a high potency of killing cancer cells in vitro. With a high aqueous solubility and coulombic interaction with cell membrane, SS–GPDs may have great potential in gene/drug delivery fields.
研究领域:
生物材料学
·
分子生物学
·
纳米医学
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF POLYMER SCIENCE PART A-POLYMER CHEMISTRY
·
2017
·Vol. 55
·期 16
·2594-2600
·
IF 2.952
Yali Luo,Jun Liu,Yunfei Liu,Yinong Lyu
Two porous porphyrin-based covalent triazine frameworks (PCTFs), in which porphyrin is incorporated as building block, have been synthesized by the Friedel–Crafts reaction. The copolymer PCTFs show large Brunauer–Emmett–Teller specific surface area of up to 1089 m 2 g −1 , high CO 2 uptake capacity reaching 139.9 mg g −1 at 273 K/1.0 bar, and good selectivity for CO 2 /CH 4 adsorption attaining 6.1 at 273 K/1.0 bar. The resulting porous solids also can be used as matrices for drug delivery of ibuprofen in vitro. © 2017 Wiley Periodicals, Inc. J. Polym. Sci., Part A: Polym. Chem. 2017 , 55 , 2594–2600
研究领域:
材料科学
·
环境科学
·
药学
✓ 已验证
产品关联
DOI
高影响因子
CURRENT PHARMACEUTICAL BIOTECHNOLOGY
·
2024
·
IF 2.2
Li Xu,Zhaohe Huang,Xiaojing Pei,Ze Zhang,Shujing Li,Yifan He
Introduction: Liposomes were extensively used for cosmetics and pharmaceuticals due to their versatility, biocompatibility, and biodegradability, as well as the ability to encapsulate water-soluble and fat-soluble substances. However, some challenges remain unsolved, including poor stability, complex preparation process, limited encapsulation efficiencies (EE%) and drug loading capacity (DLC%). Method: We herein prepared universal liquid proliposomes by rotary evaporation method and optimized formulations with different pH, glycerol content, ethanol content and preparation process. Result: The EE% of water-soluble substances was above 85%, and the maximum DLC% was 37.5%. In 7 different conditions, the optimal formulation of the proliposomes remained stable over 60 days. The excellent stability of proliposomes and nicotinamide liposomes and their essence, when applied to cosmetic formulations, was confirmed by the Turbiscan stability analyzer. Conclusion: The proposed universal liquid proliposomes can form liposomes encapsulating a variety of water-soluble substances rapidly, making them an accessible and versatile tool for improving the stability and applicability of water-soluble raw materials.
研究领域:
药剂学
·
生物材料
·
化妆品科学
·
药物输送
·
制剂工程
✓ 已验证
DOI
PubMed
高影响因子
ACS Applied Polymer Materials
·
2025
·
IF 4.7
Lida Pan,Xuepeng Li,Hang Li,Xingbo Qin,Wangqing Wu
Polymer microneedles (MNs) attract considerable attention due to their sound biocompatibility and low manufacturing cost. In this study, we prepared polypropylene (PP) MNs utilizing ultrasonic plasticization microinjection molding (UPMIM) technology, and the compression property, piercing performance, and drug infiltration promotion effect of the products were investigated. In addition, we prepared drug-loaded MNs using UPMIM technology and the dip coating method to reveal their drug loading and release properties. Meanwhile, the photothermal properties of polydopamine (PDA) MNs and their in vivo biological application performance in mice were explored. Results showed that PP MNs have good compressive toughness and piercing performance. They can pierce through mice skin, demonstrating good capability in drug infiltration promotion. The drug loading capacity of MNs rose with the increase of the PVA and sucrose contents and dropped with the rise of the temperature, indicating a fast drug release feature. Moreover, PDA MNs showed relatively strong photosensitivity and good cyclic photothermal properties as well as ideal biological application performance, with the mice skin temperature reaching 21.9 °C in 3 min. This research will provide important theoretical and technical support for the manufacturing of polymer MNs and their biological application.
研究领域:
生物医学工程
·
高分子科学
·
药剂学技术
·
材料科学
✓ 已验证
产品关联
DOI
高影响因子
PARTICLE & PARTICLE SYSTEMS CHARACTERIZATION
·
2018
·Vol. 35
·期 4
·1700447
·
IF 4.384
Lin Dai,Weiyan Zhu,Rui Liu,Chuanling Si
Self-nanoemulsifying drug delivery system (SNEDDS) is recently studied for enhancing the bioavailability of hydrophobic drugs, such as resveratrol (RSV). However, the functional design of SNEDDS for the drug structural protection is not studied yet. Here, this paper presents an efficient approach by adding lignin (a kind of abundant biomass resource) to enhance the stability of trans -RSV and meantime improve its oral bioavailability. Higher stability of trans -RSV (just decreased 2% to cis -RSV after 1 h under direct sunlight) is observed after loaded by lignin-containing SNEDDS (RSV/SLS SNEDDS). Low toxicity, high transfer efficiency (apparent permeability coefficient >1 × 10 −7 cm s −1 ), and bioavailability (1.371%) of RSV/SLS SNEDDS is successfully demonstrated in Caco-2 cells and rat model, respectively. This study serves to illustrate a simple, versatile, environmental, and economic sustainability approach to the development of nanodelivery systems for light instability drugs.
研究领域:
药剂学
·
药物传递
·
生物医学工程
·
天然产物化学
✓ 已验证
DOI
高影响因子
JOURNAL OF CONTROLLED RELEASE
·
2017
·
IF 7.786
Xiaochang Liu,Peng Quan,Shanshan Li,Chao Liu,Yuan Zhao,Yongshan Zhao,Liang Fang
Chemical enhancers are widely used for facilitating drug penetration in transdermal drug delivery system (TDDS). However, there is a lack of knowledge about how the enhancement effect changes over time. In this study, on the basis of kinetic parameters of enhancement effect, molecular details of the dynamic enhancement process was described and a new hypothesis of the recovery mechanism of the skin barrier function was proposed. Using pretreated skin and flurbiprofen patch, the effects of Azone (AZ) and menthyl decanoate (MT-10) were evaluated with in vitro permeation experiment and further confirmed by confocal laser scanning microscopy (CLSM) and TEWL. The results showed that the enhancement ratio ( ER ) increased firstly, then reached a plateau and finally decreased. The enhancement effect of MT-10 was slower ( T onset, MT-10 > T onset, AZ ), weaker ( ER max, MT-10 < ER max, AZ ) and shorter ( T eff, MT-10 < T eff, AZ ) than that of AZ. According to the results of CLSM, ATR-FTIR and molecular dynamic simulation, the dynamic enhancement effect was caused by the variation of the diffusion coefficient of intercellular lipid in the stratum corneum (SC), which was dependent on the affinity between enhancers and lipid. Moreover, the skin barrier function recovered although a large amount of enhancers still existed in the SC. Additionally, according to the results of ATR-FTIR, molecular docking and skin retention study, the dynamic effect of AZ on the skin protein only induced skin irritation but showed no influence on drug penetration, so did the amount of the enhancer. In conclusion, dynamic enhancement effect was caused by the dynamic effect of the enhancer on the SC intercellular lipid, and the skin barrier function recovered by accepting the enhancer as a new component of the lipid bilayer .
研究领域:
药剂学
·
生物医学工程
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
·
2018
·
IF 1.883
Mengyuan Cao,Xu Xue,Xixi Pei,Yiwen Qian,Lan Liu,Lili Ren,Guoguang Chen
The present research indicated that a new self-microemulsifying drug delivery systems (SMEDDS) were used to reduce the food effect of poorly water-soluble drug cinacalcet and enhance the bioavailability in beagle dogs by oral gavage. Ethyl oleate, OP-10, and PEG-200 was selected as the oil phase, surfactant and co-surfactant of cinacalcet-SMEDDS by the solubility and phase diagram studies. Central Composite Design-Response Surface Methodology was used to determine the ratio of surfactant and co-surfactant, the amount of oil for optimizing the SMEDDS formation. The prepared formulations were further characterized by the droplet size, self-microemulsifying time, zeta potential, polydispersity index (PDI), and robustness to dilution. The in vitro release profile of cinacalcet-SMEDDS was determined in four different release medium and in fasted state and fed state of simulated gastrointestinal fluid. Cinaclcet-SMEDDS were implemented under fed and fasted state in dogs and product REGPARA® was used as a comparison to the prepared formulation in the pharmacokinetics. The result showed the components of SMEDDS, the amount of oil, the ratio of surfactant, and co-surfactant was optimized using solubility, pseudo-ternary phase diagram studies, and response surface methodology. In vitro drug release studies indicated that the cinacalcet-SMEDDS eliminated the effect of pH variability in release medium and variational gastroenteric environments with improved drug release performance. Pharmacokinetic studies revealed that the profiles of cinacalcet-SMEDDS were similar both in the fasted and fed state compared with commercial product, indicating the formulation significantly promoted the absorption, enhanced bioavailability and had no food effect essentially. It is concluded that poorly water-soluble drug cinacalcet was improved in the solubility and bioavailability by using a successful oral dosage form the SMEDDS, and eliminated food effect as well.
研究领域:
药剂学
·
药物代谢
·
生物制药
✓ 已验证
产品关联
DOI
PubMed
高影响因子
AAPS PHARMSCITECH
·
2014
·Vol. 15
·期 3
·731-740
·
IF 1.776
Zhang Jianbin,Lv Yan,Zhao Shan,Wang Bing,Tan Mingqian,Xie Hongguo,Lv Guojun,Ma Xiaojun
The objective of this study is to investigate the effect of lipolysis on the release of poorly water-soluble drug from SMEDDS in the perspective of drug core/shell location. For this purpose, four SMEDDS formulations with various core/shell properties were developed based on long-chain lipid or medium-chain lipid as well as different surfactant/oil ratios. Poorly water-soluble drugs, hymecromone and resveratrol, were significantly solubilized in all SMEDDS formulations and the diluted microemulsions. Fluorescence spectra analysis indicated that hymecromone was mainly located in the shell of microemulsions, while resveratrol was located in the core. The effect of lipolysis on the release rates of drugs with different core/shell locations were investigated by a modified in vitro drug release model. For the drug located in the shell, hymecromone, the release profiles were not affected during the lipolysis process and no significant differences were observed among four formulations. For the drug located in the core, resveratrol, the release rates were increased to various degrees depending on the extent of digestion. In conclusion, the drug core/shell location plays an important role for determining the effect of lipolysis on drug release from SMEDDS formulation.
研究领域:
药剂学
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Journal of Macromolecular Science Part A-Pure and Applied Chemistry
·
2025
·
IF 2.4
Wenna Dong,Long Fang,Jinhai Ma
As a drug delivery system with vast potential applications, hydrogels have garnered significant attention due to their unique drug loading mechanisms and effectiveness. In this paper, a novel reversible thermosensitive hydrogel polymer, synthesized through copolymerization of mono-6-allyl-β-cyclodextrin, N-isopropylacrylamide, and acrylamide, is introduced. This hydrogel polymer formed a three-dimensional network structure in water, featuring β-cyclodextrin hydrophobic cavities. The encapsulated drug molecules could be slowly and progressively released from both the three-dimensional network and the β-cyclodextrin hydrophobic cavities. IR and XRD analysis confirmed the successful encapsulation of the target drug molecules, sodium salicylate and naproxen sodium, within the β-cyclodextrin cavity of the hydrogel polymer and its three-dimensional network space. Specifically, when the mass ratio of N-isopropylacrylamide/acrylamide/mono-6-allyl-β-cyclodextrin was 9.8/0.2/0.5, the polymer hydrogel demonstrated an initial gelation temperature of 34.9 °C and a final gelation temperature of 37 °C. The expansion rate of the blank hydrogel was slightly higher than that of the drug-loaded hydrogel. Both drugs undergo sustained release through the hydrogel, adhering to Fick’s diffusion law, ensuring consistent drug release within 8 h and maintaining this release for over 24 h, regardless of the drug loading rate. Within 30 days, the degradation rate of the drug-loaded hydrogels in PBS exceeded 15%, while the degradation rate in the presence of lysozyme was more than 40%. These properties render the hydrogel a versatile candidate for targeted drug delivery and biomedical applications, offering novel strategies for treating chronic diseases and other conditions.
研究领域:
生物医学工程
·
高分子科学
·
药剂学
·
材料科学
·
药物传递系统
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）