Preparation and Characterizations of RSPP050-Loaded Polymeric Micelles Using Poly(ethylene glycol)-&lt;i&gt;b&lt;/i&gt;-Poly(ε-caprolactone) and Poly(ethylene glycol)-&lt;i&gt;b&lt;/i&gt;-Poly(D,L-lactide)

Eawsakul, Komgrit; Chinavinijkul, Panarin; Saeeng, Rungnapha; Chairoungdua, Arthit; Tuchinda, Patoomratana; Nasongkla, Norased

doi:10.1248/cpb.c16-00871

Cited by 24 publications

(8 citation statements)

References 41 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…An MTT assay was used to measure cell viability. Briefly, cells were treated as described above, then incubated for 4 h at 37 °C with a 1 mg/mL MTT solution [ 43 , 44 ]. The purple formazan crystals were dissolved in DMSO when the medium was removed.…”

Section: Methodsmentioning

confidence: 99%

The Cholesterol-Modulating Effect of the New Herbal Medicinal Recipe from Yellow Vine (Coscinium fenestratum (Goetgh.)), Ginger (Zingiber officinale Roscoe.), and Safflower (Carthamus tinctorius L.) on Suppressing PCSK9 Expression to Upregulate LDLR Expression in HepG2 Cells

Ongtanasup

Prommee

Jampa

et al. 2022

Plants

Self Cite

View full text Add to dashboard Cite

PCSK9 is a promising target for developing novel cholesterol-lowering drugs. We developed a recipe that combined molecular docking, GC-MS/MS, and real-time PCR to identify potential PCSK9 inhibitors for herb ratio determination. Three herbs, C. tinctorius, C. fenestratum, and Z. officinale, were used in this study. This work aimed to evaluate cholesterol-lowering through a PCSK9 inhibitory mechanism of these three herbs for defining a suitable ratio. Chemical constituents were identified using GC-MS/MS. The PCSK9 inhibitory potential of the compounds was determined using molecular docking, real-time PCR, and Oil red O staining. It has been shown that most of the active compounds of C. fenestratum and Z. officinale inhibit PCSK9 when extracted with water, and C. fenestratum has been shown to yield tetraacetyl-d-xylonic nitrile (27.92%) and inositol, 1-deoxy-(24.89%). These compounds could inhibit PCSK9 through the binding of 6 and 5 hydrogen bonds, respectively, while the active compound in Z. officinale is 2-Formyl-9-[.beta.-d-ribofuranosyl] hypoxanthine (4.37%) inhibits PCSK9 by forming 8 hydrogen bonds. These results suggest that a recipe comprising three parts C. fenestratum, two parts Z. officinale, and one part C. tinctorius is a suitable herbal ratio for reducing lipid levels in the bloodstream through a PCSK9 inhibitory mechanism.

show abstract

Section: Methodsmentioning

confidence: 99%

The Cholesterol-Modulating Effect of the New Herbal Medicinal Recipe from Yellow Vine (Coscinium fenestratum (Goetgh.)), Ginger (Zingiber officinale Roscoe.), and Safflower (Carthamus tinctorius L.) on Suppressing PCSK9 Expression to Upregulate LDLR Expression in HepG2 Cells

Ongtanasup

Prommee

Jampa

et al. 2022

Plants

Self Cite

View full text Add to dashboard Cite

show abstract

“…Nicole Lecot, Gonzalo Rodríguez, Valentina Stancov, Marcelo Fernández, Mercedes González, Romina J. Glisoni, Pablo Cabral, Hugo Cerecetto, lack of lymphatic drainage. The EPR could allow the extravasation of nanomaterials and their accumulation inside the pathological site (Eawsakul et al, 2017;Maeda et al, 2000).…”

Section: Development Of Fluorescent-and Radiotraceable T1307-polymeri...mentioning

confidence: 99%

Development of fluorescent- and radio-traceable T1307-polymeric micelles as biomedical agents for cancer diagnosis: biodistribution on 4T1 tumor-bearing mice

Lecot

Rodríguez

Stancov

et al. 2022

Braz. J. Pharm. Sci.

View full text Add to dashboard Cite

In recent years, nanocarriers have been studied as promising pharmaceutical tools for controlled drug-delivery, treatment-efficacy follow-up and disease imaging. Among them, X-shaped amphiphilic polymeric micelles (Tetronic®, poloxamines) display great potential due to their biocompatibility and non-toxic effects, among others. In the present work, polymeric micelles based on the T1307 copolymer were initially decorated with a 4,4-difluoro-4-bora-3a,4a-diazas-indacene (BODIPY)-fluorophore in order to determinate its in vivo biodistribution on 4T1 tumor-bearing mice. However, unfavorable results with this probe led to two different strategies. On the one hand, the BODIPY-loaded micelles, L-T1307-BODIPY, and on the other hand, the 99m Tc-radiolabeled micelles, L-T1307-99m Tc, were analyzed separately in vivo. The results indicated that T1307 accumulates mainly in the stomach, the kidneys, the lungs and the tumor, reaching the maximum organ-accumulation 2 hours after intravenous injection. Additionally, and according to the results obtained for L-T1307-99m Tc, the capture of the polymeric micelles in organs could be observed up to 24 hours after injection. The results obtained in this work were promising towards the development of new radiotracer agents for breast cancer based on X-shaped polymeric micelles.

show abstract

“…Micelles. MUC-30-loaded polymeric micelles were fabricated by the film sonication method [12,27]. MUC-30 and the polymer were dissolved in tetrahydrofuran (THF).…”

Section: Preparation Of Muc-30-encapsulated Polymericmentioning

confidence: 99%

“…To overcome these obstacles, a polymeric micelle from block copolymers was employed to encapsulate MUC-30 within the core. Encapsulation of drugs in these block copolymeric micelles including poly(ethylene glycol)-b-poly (D, L-lactide) (PEG-b-PLA) and poly(ethylene glycol)-b-poly (ε-caprolactone) (PEG-b-PCL) [11] has been proved to increase water solubility of drugs [12] and prevent the development of drug resistance inhibiting ABC-transporter-mediated drug efflux [13][14][15]. ese micelles were proved to be safe in animals [16].…”

Section: Introductionmentioning

confidence: 99%

Preparation and Characterization of MUC-30-Loaded Polymeric Micelles against MCF-7 Cell Lines Using Molecular Docking Methods and In Vitro Study

Nasongkla

Tuchinda

Munyoo

et al. 2021

Evidence-Based Complementary and Alternative Medicine

Self Cite

View full text Add to dashboard Cite

MUC-30 is a hydrophobic compound which is active against the MCF-7 cancer cell line. In this study, MUC-30 was loaded in polymeric micelles to improve the water solubility and release rate. For prolonged MUC-30 release, MUC-30 was encapsulated in polymeric micelles using PEG-b-PLA and PEG-b-PCL as materials. Micelles prepared with 1 : 9 w per w ratios by film hydration achieved the highest entrapment efficiency (EE%). The EE% of MUC-30-loaded PEG-b-PCL micelles was approximately 30% greater than that of PEG-b-PLA micelles, due to the different H-bond formations between MUC-30 and the polymer membrane (PCL, 4; PLA, 3). The cytotoxic activity of MUC-30 against EGFR theoretically presented 399.31 nM (IC50 = 282.26 ng/mL) by molecular docking. In vitro cytotoxic activity of MUC-30 was confirmed by MTT assay. MUC-30 (IC50 = 11 ± 0.39 ng/mL) showed three-fold higher activity over MUC-30-loaded PEG-b-PLA micelles (IC50 = 37 ± 1.18 ng/mL) and two-fold higher over PEG-b-PCL micelles (IC50 = 75 ± 3.97 ng/mL). This was due to the higher release rate of MUC-30 from PEG-b-PLA micelles compared to PEG-b-PCL micelles. Therefore, MUC-30-loaded PEG-b-PLA micelles could be a promising candidate for breast cancer chemotherapy.

show abstract

Preparation and Characterizations of RSPP050-Loaded Polymeric Micelles Using Poly(ethylene glycol)-<i>b</i>-Poly(ε-caprolactone) and Poly(ethylene glycol)-<i>b</i>-Poly(D,L-lactide)

Abstract: RSPP050 (AG50) is one of the semi-synthetic andrographolide that is isolated from

Cited by 24 publications

References 41 publications

The Cholesterol-Modulating Effect of the New Herbal Medicinal Recipe from Yellow Vine (Coscinium fenestratum (Goetgh.)), Ginger (Zingiber officinale Roscoe.), and Safflower (Carthamus tinctorius L.) on Suppressing PCSK9 Expression to Upregulate LDLR Expression in HepG2 Cells

The Cholesterol-Modulating Effect of the New Herbal Medicinal Recipe from Yellow Vine (Coscinium fenestratum (Goetgh.)), Ginger (Zingiber officinale Roscoe.), and Safflower (Carthamus tinctorius L.) on Suppressing PCSK9 Expression to Upregulate LDLR Expression in HepG2 Cells

Development of fluorescent- and radio-traceable T1307-polymeric micelles as biomedical agents for cancer diagnosis: biodistribution on 4T1 tumor-bearing mice

Preparation and Characterization of MUC-30-Loaded Polymeric Micelles against MCF-7 Cell Lines Using Molecular Docking Methods and In Vitro Study

Contact Info

Product

Resources

About