INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2023
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IF 8.2
Yinglan Li,Jie Xu,Qingran Guan,Huaizhen Zhang,Zhuang Ding,Qingpeng Wang,Zhengping Wang,Jun Han,Min Liu,Yanna Zhao
Solid dispersions (SDs) possess the potential to enhance the bioavailability of insoluble active pharmaceutical ingredients (APIs) by effectively converting them into amorphous state. However, SDs have a tendency to recrystallize unless appropriate excipients are employed. The objective of this study was to evaluate the ability of hypromellose acetate succinate HF (HPMCAS-HF) and Soluplus® to inhibit the recrystallization of β-carotene and improve its in vivo bioavailability through the fabrication of ternary β-carotene solid dispersions (SDs) with the aid of specific surfactant. Due to rapid micellization , the dissolution profiles of β-carotene SDs based on HPMCAS-HF/Span 20 (5:5, w/w) or Soluplus®/Span 20 (6:4, w/w) combinations exhibited significant improvement, which were almost 7–10 times higher than β-carotene bulk powder. DSC and PXRD analysis indicated a notable reduction in the crystallinity degree of β-carotene within the SDs. The stability study demonstrated a half-life of β-carotene in the SDs exceeding 30 days. Additionally, the in vivo pharmacokinetics analysis confirmed that the cellulose derivatives/surfactant combinations significantly enhanced the bioavailability of β-carotene by 1.37-fold and 2.3-fold, respectively. Notably, the HPMCAS-HF/Span 20 combination exhibited superior performance. Consequently, the HPMCAS-HF/Span 20 combination held potential for the advancement of an effective drug delivery system for β-carotene.
研究领域:
药剂学
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生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF PHARMACEUTICAL SCIENCES
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2021
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IF 3.534
Yiru Wang,Yudan Fang,Feng Zhou,Qi Liang,Yueyi Deng
HPMCAS-HF, HPMCAS-MF and HPMCAS-LF were used as carriers to prepare the amorphous solid dispersions (ASDs) of quercetin (Que) by co-precipitation. The Que ASD based on PVP K30 was prepared by solvent evaporation method. The ability of polymer to inhibit Que crystallization was evaluated. The study found the order of the ability of polymer to inhibit Que nucleation to be: HF > MF > LF > K30, and that to maintain Que supersaturation to be: HF > K30 > MF > LF. The prepared solid dispersions were characterized by IR, DSC and PXRD. Although HF was the most effective crystallization inhibitor, the release of the Que/HF ASD was poor and assigned to the carrier-controlled dissolution for the strong interactions between Que and HF. The Que/MF ASD exhibited better dissolution behavior compared to the Que/K30 ASD. The dissolution behavior of the Que ASD depended on the polymer-Que interactions and the ability of crystallization inhibition of the polymer.
研究领域:
药剂学
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药物传递系统
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生物医学工程
✓ 已验证
DOI
高影响因子
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
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2019
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IF 3.532
Qiang Li,Qianqian Zhao,Qiufang Jing,Xiaosi Ma,Ning Chen,Guobin Ren,Defang Ouyang,Fuzheng Ren
Molecular interactions between drug and polymeric carriers are believed to be the key for high drug loading and better physical stability of micro-particles. However, molecular interactions between drug and polymer are still difficult to investigate using only experimental tools. In this study, high-loaded glipizide (GLP)/hydroxypropyl methylcellulose acetate succinate (HPMCAS) (1/1 w/w) micro-particles were prepared using an in situ pH-dependent solubility method. Molecular interactions within the micro-particles were investigated by integrated experimental and modeling techniques. The dissolution rate of GLP/HPMCAS micro-particles was significantly better than those of solid dispersions and physical mixtures. Scanning electron microscopy images showed that the polymer inhibited GLP recrystallization. Experimental (FTIR spectroscopy, differential scanning calorimetry , powder X-ray diffraction and nuclear magnetic resonance spectroscopy) and molecular dynamics simulation revealed that hydrogen-bonding was the key to the properties of the micro-particles. Our research developed high drug-loading GLP/HPMCAS micro-particles and investigated the interactions between drug and polymer at the molecular level. This integrated approach could be practical methodology for future formulation design.
研究领域:
药剂学
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分子生物学
✓ 已验证
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2024
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IF 7.7
Yinglan Li,Qipeng Wei,Jianshuo Su,Huaizhen Zhang,Zhiping Fan,Zhuang Ding,Min Wen,Min Liu,Yanna Zhao
In this study, the interaction among multifunctional excipients, including polysaccharides, cellulose derivatives, and surfactants, was particularly investigated, together with its impact on the physicochemical properties of astaxanthin amorphous solid dispersions (ASTX ASDs). It was indicated that Span 20 could rapidly form hemimicelles or aggregates in the presence of hypromellose acetate succinate HF (HPMCAS-HF, HF) or Soluplus®, while octenyl succinic anhydride modified starch (OSA-starch) efficiently assisted in the coalescence inhibition of drug-excipients aggregates, which was jointly beneficial to the recrystallization inhibition of amorphous ASTX. ASTX ASDs were further prepared with OSA-starch, HPMCAS-HF/Soluplus®, and Span 20 as the wall materials. DSC, SEM, and XRD confirmed that crystalline ASTX had transformed to amorphous state in the ASDs, while FT-IR spectra provided evidence suggesting the existence of hydrogen bonds and hydrophobic interaction between ASTX and the excipients. The dissolution of ASTX ASDs in different media revealed significant promotion, while the pharmacokinetic results further demonstrated the oral bioavailability of ASTX ASDs enhanced remarkably, exhibiting 2.75-fold (SD 1 ) and 1.87-fold (SD 2 ) increase, respectively, compared to ASTX bulk powder. In summary, the cellulose derivatives-surfactant interaction had great impact on the physicochemical properties of ASTX ASDs, and their combinations exhibited great potential for delivering the hydrophobic bioactive compounds efficiently.
研究领域:
药学
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材料科学
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药理学
✓ 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）