JOURNAL OF BIOMATERIALS APPLICATIONS
·
2024
·
IF 2.3
Xuena Zhang,Xuehan Wang,Juan Xu,Ting Wang
Drospirenone (DROP) is a highly effective, low-toxicity, safe new generation progestin that counteracts estrogen-related sodium retention, is well tolerated, and has a positive effect on premenstrual syndrome (PMS). However, the low water solubility of DROP and its chemical instability resulted in low bioavailability. In this study, we developed a two-step delivery system to enhance drospirenone’s solubility and stability. We prepared a drospirenone liposome complex to optimize the encapsulation process and achieve an encapsulation efficiency of (84.9 ± 0.73) %, with an 878-fold increase in solubility under optimal conditions. To address the instability of high drug-loading liposomes, we immobilized the drospirenone liposome inclusion complex using a cellulose-based hydrogel. The system achieved uniform loading of liposomes in the hydrogel, as confirmed by SEM and FTIR analysis. 0.5 g hydrogel can be loaded with up to 96.48 mg drospirenone, and the encapsulation efficiency is (80.4 ± 1.17%). It was indicating the potential for wider application of drospirenone with enhanced water solubility and improved stability. At the same time, it also provides support for sustained-release systems or large dose drug delivery.
研究领域:
药剂学
·
药物递送系统
✓ 已验证
DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
·
2017
·
IF 4.159
Hong Wang,Guangxing Zhang,Xueqin Ma,Yanhua Liu,Jun Feng,Kinam Park,Wenping Wang
Poly (lactide-co-glycolide) (PLGA) microparticles are widely used for controlled drug delivery. Emulsion methods have been commonly used for preparation of PLGA microparticles, but they usually result in low loading capacity, especially for drugs with poor solubility in organic solvents . In the present study, the nanocrystal technology and a water-soluble polymer template method were used to fabricate nanocrystal-loaded microparticles with improved drug loading and encapsulation efficiency for prolonged delivery of breviscapine . Breviscapine nanocrystals were prepared using a precipitation-ultrasonication method and further loaded into PLGA microparticles by casting in a mold from a water-soluble polymer. The obtained disc-like particles were then characterized and compared with the spherical particles prepared by an emulsion-solvent evaporation method. X-ray powder diffraction (XRPD) and confocal laser scanning microscopy (CLSM) analysis confirmed a highly-dispersed state of breviscapine inside the microparticles. The drug form, loading percentage and fabrication techniques significantly affected the loading capacity and efficiency of breviscapine in PLGA microparticles, and their release performance as well. Drug loading was increased from 2.4% up to 15.3% when both nanocrystal and template methods were applied, and encapsulation efficiency increased from 48.5% to 91.9%. But loading efficiency was reduced as the drug loading was increased. All microparticles showed an initial burst release, and then a slow release period of 28 days followed by an erosion-accelerated release phase, which provides a sustained delivery of breviscapine over a month. A relatively stable serum drug level for more than 30 days was observed after intramuscular injection of microparticles in rats. Therefore, PLGA microparticles loaded with nanocrystals of poorly soluble drugs provided a promising approach for long-term therapeutic products characterized with preferable in vitro and in vivo performance.
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
FOOD HYDROCOLLOIDS
·
2018
·
IF 5.089
Mingyu Ji,Xinyu Sun,Xiaoban Guo,Wenjin Zhu,Jiulin Wu,Li Chen,Jianhua Wang,Mingmao Chen,Cui Cheng,Qiqing Zhang
As a natural preservative, cinnamaldehyde (CA) has a bright application prospect. However, CA is sensitive to light and can be easily oxidized. What's more, its water solubility is poor. These properties greatly limit its application. In this study, CA/sodium alginate (SA)/chitosan (CS) nanoparticles (CA/SA/CS NPs) were prepared by using SA and CS as wall materials, and CA as core material. The single factor experiment showed that the optimal CA/SA/CS NPs can be obtained when the mass ratio of SA to CS was 5.5/1, SA to CaCl 2 was 5/1, SA to CA was 1/2, and the pH of CS solution was 5.0. Under this condition, the average size of the prepared nanoparticles was 455.2 nm, polymer dispersity index (PDI) value was 0.189, zeta potential was −40.8 mV, and the encapsulation efficiency was 72.92%. The scanning electron microscopy (SEM) and atomic force microscopy (AFM) images confirmed the formation of nanoparticles, which were spherical or ellipsoidal in shape. The fourier transform infrared spectroscopy (FTIR) and multifunctional polycrystalline X-ray diffraction (XRD) spectra indicated that CA was encapsulated in the nanoparticles. Furthermore, in vitro release experiments showed that CA/SA/CS NPs had the function of sustained release. In summary, SA/CS NPs can be used as a promising carrier for CA.
研究领域:
材料科学
·
纳米技术
·
药学
·
食品科学
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF LIPOSOME RESEARCH
·
2019
·
IF 2.507
Zeyu Wu,Tingting Wang,Yonghong Song,Yang Lu,Tianyun Chen,Pengpeng Chen,Ailing Hui,Yan Chen,Haixiang Wang,Wencheng Zhang
The purpose of this study was to optimize the preparation conditions of podophyllotoxin liposomes (PPT-Lips), and to investigate their effects on PC3 cells. PPT-Lips were prepared by using a thin-film dispersion method. In order to achieve maximum drug encapsulation efficiency (EE), the process and formulation variables were optimized by response surface methodology (RSM). The optimum preparation conditions were cholesterol to lecithin ratio of 3.6:40 (w/w), lipid to drug ratio of 15.8:1 (w/w), and the ultrasonic intensity of 35% (total power of 400 W). The experimental EE of PPT-Lips was 90.425%, which was consistent with the theoretically predicted value. The characterization studies showed that PPT-Lips were well-dispersible spherical particles with an average size of 106 nm and a zeta potential of –10.1 mV. A gradual and time-dependent pattern of PPT from liposomes was found in in vitro drug release with a cumulative release amount up to 70.3% in 24 h. Results of cell viability experiments on PC3 cells demonstrated that PPT-Lips exhibited more effective anticancer activity in comparison with free PPT. Therefore, PPT-Lips represent an efficient and promising drug delivery system for PPT.
研究领域:
药剂学
·
肿瘤学
·
药物递送
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ACS Omega
·
2025
·
IF 4.3
Shixi Li,Xuhua Liang,Jiale Xing,Min Cheng,Xue Liu,Rong Zheng,Ruya Feng
Phillyrin has many effects, such as reducing blood lipids, anti-inflammatory properties, lowering blood pressure, and decreasing tyrosinase activity. However, the bioavailability of phillyrin with oral administration is very low due to its poor water solubility. In order to overcome the bioavailability problems of phillyrin, a phillyrin self-microemulsion was prepared by changing the dosage form, the preparation process of which was optimized, and its characterizations were investigated. Based on a self-microemulsion administration system, appropriate ingredients were chosen first on the basis of a solubility test, and the range of application of each ingredient was determined by ternary phase diagrams. Second, the formula of the phillyrin self-microemulsion was optimized through the response surface method by using the mass percentage of ethyl oleate and Km value (the ratio between surfactant and cosurfactant) as independent variables and using the encapsulation efficiency (EE), grain size, and polydispersity index (PDI) as dependent variables. The average grain size, PDI, and encapsulation efficiency of the optimized microemulsion are 42.37 nm, 0.244, and 69.51%, respectively. Finally, the apparent properties, stability, and pharmic content of the prepared phillyrin self-microemulsion were characterized. Moreover, in vitro dissolution was analyzed by using the rotatory-basket method, proving the self-microemulsion could improve the in vitro dissolution of phillyrin. The above-mentioned results indicated that self-microemulsion could be used to improve the solubility and bioavailability of phillyrin, which might be a good alternative solution to improve the oral utilization of phillyrin.
研究领域:
药剂学
·
药物递送
·
分子药理学
·
药物代谢
·
纳米医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
·
2019
·
IF 4.708
Jiwei Liu,Yan Xu,Zhe Liu,Hao Ren,Zhengjie Meng,Kuntang Liu,Zhangya Liu,Jiahui Yong,Yonglu Wang,Xueming Li
Poor encapsulation and high initial burst were two major obstacles for the water-soluble peptide drug loaded microspheres preparation using the industrial emulsification method. In the present study, we hypothesized that the hydrophobic ion-pairing (HIP) complex strategy with a further healing of the pores within the microspheres may improve drug encapsulation and initial burst release. DSS was chosen as the most suitable one among the three test ion-pairing agents (SDS, DSS and STC) due to its high binding efficiency with drug and reversible dissociation capacity in presence of counter ions. The formation of HIP complex between octreotide acetate and DSS successfully reversed the highly water-soluble nature of the drug. A specific S/O/W method was adopted to encapsulate such drug containing HIP complex. The encapsulation efficiency of the drug was greatly improved compared with the conventional W1/O/W2 method (from 44% to 90%). Under the optimal healing conditions (the healing time 6 h, temperature 40 °C and 4% DEP content), the pores within the microspheres were effectively healed. Initial burst amount of octreotide acetate in S/O/W microspheres decreased to 3.56%. The pore healing effect was further confirmed by the scanning electron microscopy and fluorescence microscopy results. In the process of testing the drug release performance of such new strategy in vitro and in vivo, a more satisfactory single phase release profile with sustained and steady drug release was observed. These results suggested that the modified HIP strategy could be a promising platform for water-soluble peptide encapsulation with high encapsulation efficiency, low initial burst and stable drug release mechanism.
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
SAUDI JOURNAL OF BIOLOGICAL SCIENCES
·
2015
·
IF 1.257
Huibin Li,Fang Chen
The aim of this work was to prepare coenzyme Q10 (CoQ10) long-circulating liposomes, and establish the quality standard to determine the content and entrapment efficiency. CoQ10 long-circulating liposomes were prepared by the film dispersion method, HPLC assay for the determination of CoQ10 was developed. Free drugs and liposomes were separated using the protamine aggregation method and entrapment efficiency was determined. The liposomes were homogeneous and the mean diameter was 166.0 nm, Zeta potential was −22.2 mV. The content and entrapment efficiency of CoQ10 were 98.2% and 93.2% for three batches of liposomes, respectively. The lyophilized form of liposomes prepared by freeze-drying showed stable quality characteristics during storage. The formulation and preparative method can be used to prepare CoQ10 long-circulating liposomes with high entrapment efficiency and high quality, the determination method of drug content and entrapment efficiency were effective and rapid and can be used for quality evaluation of liposomes.
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
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
Iranian Journal of Pharmaceutical Research
·
2025
·Vol. 24
·期 1
·e161557
·
IF 1.8
Qinfang He,Riqing Cheng,Jiahao Shi,Ta Na,Qiherima Wang,Sarangowa Ochir
Background Rosa rugosa polysaccharides (RRP), a principal active component derived from R. rugosa Thunb., exert immunomodulatory effects. However, their therapeutic application is limited by rapid metabolism, short duration of action, and low bioavailability. Objectives To optimize the preparation process of Rosa rugosa polysaccharide liposomes (RRPL) and evaluate their immune cell activation in vitro. Methods The RRPL were prepared using the reverse-phase evaporation method, with encapsulation efficiency (EE) as the primary evaluation criterion. An orthogonal test was employed to optimize the preparation parameters. Various characteristics of RRPL were assessed, including morphology, particle size, Polydispersity Index (PDI), zeta potential, cumulative release rate in vitro, and stability. The immunological effects of RRPL were evaluated through cellular assays involving mouse spleen lymphocytes, peritoneal macrophages, and bone marrow-derived dendritic cells (BMDCs). Results The RRPL demonstrated an EE of approximately 81.96%, an average drug loading (DL) capacity of 13.86%, a particle size of 124.00 nm, a PDI of 0.23, and a zeta potential of -12.97 mV. The formulated RRPL exhibited high EE and DL capacity, alongside favorable slow-release properties and stability. These enhancements led to improved drug bioavailability and prolonged duration of action. Furthermore, RRPL significantly promoted the proliferation of spleen lymphocytes; enhanced the phagocytic activity of peritoneal macrophages; increased the secretion of interleukin (IL)-6, IL-1β, and interferon (IFN)-γ; activated immature BMDCs; and induced the maturation of BMDCs, resulting in increased production of IL-12p70 and tumor necrosis factor (TNF)-α. Conclusions This study successfully developed RRPL that markedly enhance immune cell activation compared with RRP. These findings provide a theoretical foundation for further exploration and development of these liposomal formulations.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2025
·
IF 5.2
Li-Jing Lan,Lian-Bing Long,Ling-Zhi Shi,Ming-Wei Huo,Xiang-Xiang Huang,Ya-Wen Liu,Le-Yan Gu,Jing-Yi Liu,Ye-Chao Zhang,Renyu Huang,Qing-Ri Cao
The industrial scalability and clinical translation of liposomal formulations are significantly hindered by challenges in stability and batch-to-batch variability. To address these limitations, docetaxel (DTX)-loaded long-circulating liposomal freeze-dried powders were engineered via a synergistic integration of microfluidic technology and lyophilization, optimized through an orthogonal experimental design focusing on particle size, polydispersity index (PDI), and entrapment efficiency (EE). The optimized formulation, incorporating hydroxypropyl-β-cyclodextrin (HP-β-CD) as a lyoprotectant, demonstrated nanoscale particle diameter (∼120 nm), monodisperse distribution (PDI < 0.2), and elevated EE (>90 %), with physicochemical integrity preserved post-lyophilization. Reconstituted DTX liposomes (DTX-Lip) exhibited pH-dependent sustained release kinetics, with enhanced drug elution at acidic pH (5.5) versus physiological pH (7.4). Solid-state characterization (XRD, FT-IR, DSC) confirmed molecular interactions between DTX and lipid-excipient matrices. In vitro cytotoxicity assays revealed superior apoptotic induction in A549 human lung carcinoma cells by DTX-Lip compared to free DTX solution (DTX-Sol). Pharmacokinetic profiling in vivo demonstrated prolonged systemic circulation of DTX-Lip, marked by significantly elevated area under the curve (AUC 0-∞ ), maximum drug concentration (C max ), mean retention time (MRT 0-∞ ), longer half-life (T 1/2 ), lower clearance (CL) and steady-state volume of distribution (V ss ) relative to DTX-Sol (p < 0.05). In a C57BL/6 murine lung cancer model, DTX-Lip elicited significant tumor suppression (p < 0.05) without mortality, underscoring enhanced therapeutic efficacy and mitigated systemic toxicity. Collectively, the engineered DTX-Lip system combines optimal nano-pharmaceutical attributes (size, homogeneity, EE), controlled release, and favorable in vitro-in vivo performance, offering a robust platform for industrial-scale production of stable, efficacious liposomal DTX formulations. These findings advance translational strategies for liposome-based chemotherapeutics with improved reproducibility and clinical safety.
研究领域:
肿瘤学
·
药剂学
·
纳米医学
·
药物递送
·
药代动力学
·
转化医学
·
临床药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
REACTIVE & FUNCTIONAL POLYMERS
·
2025
·
IF 5.1
Meixue Cao,Fei Zhou,Shuan Cheng,Xinyue Wang,Ziyu Yuan,Xiuwen Huang,Zuju Shu
To explore the effects of preparation methods on the release kinetics of curcumin (Cur)-loaded sustained-release composites, three fabrication techniques—solvent casting, uniaxial electrospinning, and coaxial electrospinning—were employed to develop Cur-loaded composites using Cur as the model drug, soluble starch (St) and polyvinyl alcohol (PVA) as the matrices. The microstructure and chemical composition of three composite groups were characterized, and their functional properties were evaluated, including swelling capacity, degradation behavior, Cur loading capacity (LC), Cur encapsulation efficiency (EE), and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity. Additionally, the in vitro Cur release behavior of the composites was analyzed, and release kinetics were fitted using mathematical models. Results indicated that the preparation methods had no significant impact on the chemical composition of the Cur-loaded composites. However, the nanofibers fabricated by the coaxial electrospinning technique exhibited a unique core-shell microstructure, which distinguished them from the cast films and uniaxial electrospun membranes. Compared with the other two groups, the coaxial membrane showed higher Cur LC and EE, a higher swelling ratio, a lower degradation rate, and a stronger DPPH radical scavenging ability. Kinetic fitting revealed that the Cur release profiles of all three composite groups conformed to the First-order model, but their release performances differed significantly. The coaxial electrospun membrane outperformed the cast film and uniaxial electrospun membrane, with a Cur cumulative release rate of 51.73 % at 96 h and retained significant potential for sustained release. In conclusion, the preparation method directly regulated the antioxidant activity and sustained-release behavior of Cur in the composites. This study provides theoretical basis and technical reference for the design and development of novel drug-loaded sustained-release composite materials.
研究领域:
药物递送
·
生物材料
·
药剂学
·
高分子科学
·
抗氧化研究
✓ 已验证
产品关联
DOI
高影响因子
LANGMUIR
·
2025
·
IF 3.9
Ruoxin Wei,Jiaze Dou,Yihui Wu,Jinjin Li,Lian Cen,Zhenhao Xi
Microsphere formulations represent a promising drug delivery system for proteins and peptides with short half-lives as they effectively mitigate drug degradation in vivo. This study aimed to develop poly(lactic-co-glycolic acid) (PLGA) microspheres loaded with leuprolide acetate (LA) using microfluidic technology and to investigate key factors that could have a significant effect on the LA encapsulation and loading. A glass capillary microfluidic device for a water-in-oil-in-water (W/O/W) emulsion system was developed. Gelatin (Gel) of varying concentrations was introduced in the internal aqueous phase, and different collecting solutions for W/O/W emulsions were investigated. The effect of the LA concentration in the inner phase was also explored. It was shown that LA-loaded PLGA microspheres (LA–PLGA–MS) by microfluidics were monodisperse with a uniform particle size of 80 μm and exhibited a distinguished core–shell structure. At a Gel concentration of 7.5 mg/mL, the microspheres reached a maximum encapsulation efficiency (EE) of 80.28% and a drug loading (DL) of 4.24%. The in vitro release could last for around 28 days. The DL of microspheres was found to be increased with the increase in LA concentration in the inner water phase. The incorporation of Gel within the inner water phase and the collecting solution with a suitable pH value were the main factors that affected the EE of microspheres. Briefly, LA–PLGA–MS could be successfully prepared and regulated using microfluidics and sustained LA release as monodispersed microsphere formulations. The developed technological strategy could provide a precise strategy and experimental reference for applications in delivery systems for water-soluble peptides and proteins.
研究领域:
药剂学
·
生物医学工程
·
纳米技术
·
药物递送
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）