MATERIALS LETTERS
·
2024
·
IF 2.7
Juanping Zheng,Junzhao Su,Hongsheng Luo,Wenhui Yang,Tianhao Yu
A novel salicylic acid microsponge was prepared using the quasi-emulsion solvent diffusion method. The yield, encapsulation efficiency, morphology, thermal properties, drug state, in vitro release, and application potential were systematically evaluated. The optimized microsponges demonstrated a yield of 84.92 % and an encapsulation efficiency of 68.69 %. The morphology of the microsponges exhibited a porous spherical structure. Additionally, the interaction between salicylic acid (SA) and ethyl cellulose (EC) enhanced the thermal stability of the microsponges and significantly reduced the crystallinity of SA. These microsponges exhibited excellent sustained release characteristics, enabling drug release for up to 78 h. Finally, combining the SA microsponges with the Carbopol 934 hydrogel system demonstrated favorable viscoelasticity, creep recovery, and stability, providing new insights for its application in dermatological treatments.
研究领域:
药剂学
·
皮肤科治疗
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DOI
高影响因子
JOURNAL DE MYCOLOGIE MEDICALE
·
2025
·
IF 1.8
Zhaowei Jin,Danqing Wu,Yangnan Chen,Yanqiu Long,Yan Liu,Zhiyun Zheng,Shuangying Gui,Yuzhe Huang,Ning He
Ketoconazole (KCZ), an imidazole antifungal drug, is constrained by its low solubility and poor stability, restricting its effective absorption and bioavailability. This study introduces a KCZ-loaded microsponge based film coating agent (KCZ-MSF), designed to enhance the transdermal absorption and bioavailability of KCZ. The KCZ-MS was prepared by emulsion solvent evaporation method and the composition of the prescription was optimized by Box-Behnken design (BBD). Moreover, characterization of the optimized KCZ-MS was conducted using scanning electron microscopy (SEM), Fourier-transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC). The film coating agent's preparation was further optimized through orthogonal experiments, converting the optimized KCZ-MS into a film coating agent suitable for topical skin application. The KCZ-MS showed a spherical porous structure with a mean particle size of 22.42 ± 8.45 μm, a drug loading efficiency of 20.74%, entrapment efficiency of 92.12%, and good compatibility between the drug and excipients. The optimized KCZ-MSF displayed good physical properties. In vitro transdermal experiments revealed that the skin retention of KCZ-MSF surpassed that of commercially available KCZ cream at 6, 12, and 24 h. The pharmacokinetic experiment results indicate that the area under the curve ( AUC 0-24 ) of KCZ-MSF 420.71 ± 21.77 μg/(g·h) is 2.05 times that of KCZ film coating agent (KCZ-F) and 1.29 times that of commercially available ketoconazole cream. Therefore, KCZ-MSF presents a more promising platform for the treatment of superficial skin fungal infections.
研究领域:
药剂学
·
皮肤科学
·
药物化学
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产品关联
DOI
PubMed
高影响因子
PLoS One
·
2013
·Vol. 8
·期 11
·e79881
·
IF 3.73
Sha-Sha Li,Guo-Feng Li,Li Liu,Xiao Jiang,Bin Zhang,Zhi-Gang Liu,Xue-Ling Li,Li-Dong Weng,Ting Zuo,Qiang Liu
The aim of the present study was to design a novel topical skin-target drug-delivery system, the paeonol microsponge, and to investigate its drug-release patterns in dosage form, both in vitro and in vivo . Paeonol microsponges were prepared using the quasi-emulsion solvent-diffusion method. In vitro release studies were carried out using Franz diffusion cells, while in vivo studies were investigated by microdialysis after the paeonol microsponges were incorporated into a cream base. In vitro release studies showed that the drug delivered via microsponges increased the paeonol permeation rate. Ex vivo drug-deposition studies showed that the microsponge formulation improved drug residence in skin. In addition, in vivo microdialysis showed that the values for the area under the concentration versus time curve (AUC) for the paeonol microsponge cream was much higher than that of paeonol cream without microsponges. Maximum time (T max ) was 220 min for paeonol microsponge cream and 480 min for paeonol cream, while the half-life (t 1/2 ) of paeonol microsponge cream (935.1 min) was almost twice that of paeonol cream (548.6 min) in the skin (n = 3). Meanwhile, in the plasma, the AUC value for paeonol microsponge cream was half that of the paeonol cream. Based on these results, paeonol-loaded microsponge formulations could be a better alternative for treating skin disease, as the formulation increases drug bioavailability by lengthening the time of drug residence in the skin and should reduce side-effects because of the lower levels of paeonol moving into the circulation.
研究领域:
药剂学
·
皮肤科学
·
药物代谢动力学
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DOI
PubMed
高影响因子
AAPS PHARMSCITECH
·
2022
·Vol. 23
·期 6
·1-16
·
IF 4.026
Ma Lin,Guo Song,Piao Jingshu,Piao Mingguan
Griseofulvin (GF) is used as an antifungal to treat superficial skin fungal infections such as tinea capitis and tinea pedis. Currently, GF is only available in traditional oral dosage forms and suffers from poor and highly variable bioavailability, hepatotoxicity, and long duration of treatment. Therefore, the main objective of this study was to reduce the side effects of the drug and to increase the concentration of the drug retained in the cutaneous stratum corneum (SC) and improve its efficacy through the preparation of drug-laden GF microsponge (GFMS). The emulsification-solvent-diffusion method was used to prepare GFMS, and the prescriptions were screened by a single-factor approach. The optimized formulation (GFF8) had a microsponge particle size (μm) of 28.36 ± 0.26, an encapsulation efficiency (%) of 87.53 ± 1.07, a yield (%) of 86.58 ± 0.42, and drug release (%) from 77.57 ± 3.88. The optimized microsponge formulation was then loaded into a Carbopol 934 gel matrix and skin retention differences between the microsponge gel formulation and normal gels were examined by performing skin retention and fluorescence microscopy tests. Finally, the hepatoprotective and cutaneous stratum corneum retention abilities of microsponge gel formulations compared to oral GF formulations were assessed by hepatotoxicity, pharmacokinetics, and tissue distribution studies. This provides a new perspective on GF dermal stratum corneum retention administration. Graphical abstract
研究领域:
药剂学
·
药学
·
皮肤病学
·
毒理学
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产品关联
DOI
PubMed
高影响因子
ACS Applied Polymer Materials
·
2022
·
IF 4.855
Lu Yang,Yunhong Cong,Jingyi Zhang,Zheyuan Gu,Lili Shen,Huailing Gao,Xianyu Zheng,Mohan Wang,Jiacai He
Uniform and porous chitosan-based microparticles with injectable and shape-memory properties are particularly attractive due to their promising application potential for tissue engineering and regenerative medicine. However, simple and efficient methods for producing this kind of microparticle are still desirable. In this study, we report that uniform, injectable, and shape-memory chitosan microsponges were efficiently prepared by combining microfluidic emulsion with further freezing and in situ thawing processes without using any potentially cytotoxic chemical cross-linker. The produced chitosan microsponges have controllable size and could be easily injected with syringe needles. Structural observations confirmed that the chitosan microsponge had an interconnected porous structure with pore size of several micrometers and could withstand a large compressive strain of ∼93% and then recover ∼96% of its initial diameter without structural damage. The chitosan microsponges showed a high porosity (∼84%) and swelling ratio (∼3800%) as well as good antibacterial activity. Additionally, an in vitro cell coculturing investigation revealed that they also had good biocompatibility and exhibited great superiority to support cell adhesion and proliferation in three dimensions. The kind of chitosan microsponge presented here has great potential to serve as cell carriers for biomedical applications, especially as injectable scaffolds for regeneration and reconstruction of tissue defects.
研究领域:
组织工程
·
再生医学
·
生物医学材料
·
生物材料科学
✓ 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）