Assessment of amentoflavone loaded sub-micron particle preparation using supercritical antisolvent for its antitumor activity

2021 ◽  
Vol 18 ◽  
Author(s):  
Shulei Duan ◽  
Jingfu Jia ◽  
Biao Hong ◽  
Jie Zhou ◽  
Yi Zhang ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Drug Release ◽  
Spherical Shape ◽  
Inhibitory Effect ◽  
Supercritical Antisolvent ◽  
Micron Particle ◽  
Release Assay ◽  
Particle Preparation ◽  
Release Speed

Introduction: The amentoflavone (AMF) loaded polymeric sub-micron particles were prepared using supercritical antisolvent (SAS) technology with the aim of improving the anticancer activity of AMF. Materials and Methods: Zein and phospholipid mixtures composed of hydrogenated phosphatidylcholine (HPC) and egg lecithin (EPC) were used as carrier materials and, the effects of carrier composition on the product morphology and drug release behavior were investigated. When the mass ratio of Zein/HPC/EPC was 7/2/1, the AMF loaded particles were spherical shape and sub-micron sized around 400 nm, with a drug load of 4.3±0.3 w% and entrapment efficacy of 87.8±1.8%. The in vitro drug release assay showed that adding EPC in the wall materials could improve the dispersion stability of the released AMF in an aqueous medium, and the introduction of HPC could accelerate the drug release speed. Results: MTT assay demonstrated that AMF-loaded micron particles have an improved inhibitory effect on A375 cells, whose IC50 was 37.39μg/ml, compared with that of free AMF(130.2μg/ml). Conclusion: It proved that the AMF loaded sub-micron particles prepared by SAS were a prospective strategy to improve the antitumor activity of AMF, and possibly promote the clinical use of AMF preparations.

scholarly journals Synthesis, Characterization, and In Vitro Drug Delivery of Chitosan-Silica Hybrid Microspheres for Bone Tissue Engineering

2019 ◽  
Vol 2019 ◽  
pp. 1-7 ◽  
Author(s):  
Niu Niu ◽  
Shu-Hua Teng ◽  
Hua-Jian Zhou ◽  
Hai-Sheng Qian
Keyword(s):  
Drug Release ◽  
Sol Gel ◽  
Particle Diameter ◽  
Spherical Shape ◽  
Average Particle ◽  
High Dispersity ◽  
Model Drug ◽  
Regular Spherical Shape

Chitosan-silica (CS-SiO2) hybrid microspheres were prepared through the combined process of sol-gel and emulsification-crosslinking. Their composition, morphology, in vitro bioactivity, and drug release behavior were investigated. The results showed that, when 20 wt% SiO2 was incorporated, the as-prepared CS-SiO2 hybrid microspheres exhibited a regular spherical shape, a high dispersity, and a uniform microstructure. Their average particle diameter was determined to be about 24.0 μm. The in situ deposited inorganic phase of the hybrid microspheres was identified as amorphous SiO2, and its actual content was determined by the TG analysis. As compared with the pure chitosan microspheres, the CS-SiO2 hybrid microspheres displayed a greatly improved in vitro bioactivity. Vancomycin hydrochloride (VH) was selected as a model drug. It was demonstrated that the CS-SiO2 hybrid microspheres presented a good capacity for both loading and sustained release of VH. Moreover, the increase of the SiO2 content efficiently slowed down the drug release rate of the CS-SiO2 hybrid microspheres.

scholarly journals Synthesis, structural characterization, cytotoxicity and encapsulation studies of N,Nʹ-(1, 2-dicyano-1,2-vinylene)-bis(4-hydroxysalicylideneaminato) di(p-chlorobenzyl)tin as potential anticancer drug

2019 ◽  
Vol 42 (1) ◽  
pp. 94-101
Author(s):  
Nur Adibah Mohd Amin ◽  
Rusnah Syahila Duali Hussen ◽  
See Mun Lee ◽  
Kae Shin Sim ◽  
Suerialoasan Navanesan
Keyword(s):  
Drug Release ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Spherical Shape ◽  
Average Diameter ◽  
Diphenyltetrazolium Bromide ◽  
Ft Ir ◽  
Phosphate Buffered Saline ◽  
Mcf 7

Abstract Two new diorganotin(IV) complexes with the general formula (RC7H6)2Sn(L) (where RC7H6 = p-ClBn, C1; and p-FBn, C2) were prepared based on the reaction of 2,3-bis(4-hydroxysalicylidene-amino)-maleic nitrile (L) with substituted dibenzyltin(IV) dichloride. The structures were confirmed by elemental analysis, Fourier transform infrared (FT-IR), proton and carbon nuclear magnetic resonance (1H and 13C NMR). They were tested against several cancer cell lines by using the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. C1, which was most effective against MCF-7 breast cancer cell line, was further investigated in formulation and encapsulation studies, including drug encapsulation efficiency, particle size, morphology and in vitro drug release. An encapsulation of about 90% was achieved with particles of 128 nm average diameter. Field emission scanning electron microscopy (FESEM) confirmed a spherical shape for the encapsulated C1. The cumulative drug release over a period of 60 days in phosphate buffered saline (PBS) at pH 7.4 was 75%. Based on these results, the formulated drug has the potential of a slow release drug for cancer chemotherapy.

PEG−Doxorubicin Conjugates:  Influence of Polymer Structure on Drug Release, in Vitro Cytotoxicity, Biodistribution, and Antitumor Activity

2005 ◽  
Vol 16 (4) ◽  
pp. 775-784 ◽  
Author(s):  
Francesco M Veronese ◽  
Oddone Schiavon ◽  
Gianfranco Pasut ◽  
Raniero Mendichi ◽  
Lars Andersson ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Drug Release ◽  
Polymer Structure ◽  
In Vitro Cytotoxicity ◽  
Release In Vitro

scholarly journals Human natural killer cells can inhibit clonogenic growth of fresh leukemic cells

Blood ◽  
1983 ◽  
Vol 61 (3) ◽  
pp. 596-599 ◽  
Author(s):  
M Beran ◽  
M Hansson ◽  
R Kiessling
Keyword(s):  
Nk Cells ◽  
Natural Killer ◽  
Nk Cell ◽  
Colony Growth ◽  
Inhibitory Effect ◽  
Leukemic Cells ◽  
Target Cells ◽  
Human Natural Killer Cells ◽  
Release Assay

Abstract The effect of allogenic human natural killer (NK) cells on fresh leukemic cells from three patients was investigated. The low levels of leukemic target cell lysis in the conventional 51Cr-release assay contrasted with a pronounced inhibitory effect on the colony growth of the clonogeneic leukemic target cells (L-CFC). The ability of allogeneic lymphocytes to inhibit L-CFC increased if they were pretreated with interferon (IFN), which also increased their NK activity, monitored in parallel cytotoxicity assay, against K562. Furthermore, cell separation procedures, based on differences in density among nonadherent lymphocytes, revealed that only NK cell containing fractions were inhibitory. We have also compared the susceptibility to NK-mediated L-CFC inhibition of IFN pretreated leukemic target cells with that of nontreated target cells. As in the case of NK lysis in general, this pretreatment of target cells abolished the presumably NK-mediated L-CFC inhibition. In conclusion, these data provide the first indication that NK cells can inhibit the in vitro growth of fresh clonogenic leukemia cells from patients with nonlymphocytic leukemia. The identity of NK cells as effector is strongly suggested by Percoll separation and responsiveness to interferon; the final proof awaits more sophisticated purification of these cells.

A COMPARATIVE ASSESSMENT OF VESICULAR FORMULATIONS: TRANSFERSOMES AND CONVENTIONAL LIPOSOMES LOADED IVABRADINE HYDROCHLORIDE

2020 ◽  
pp. 51-55
Author(s):  
GITA CHAURASIA ◽  
NARENDRA LARIYA
Keyword(s):  
Drug Release ◽  
Physical Stability ◽  
Physical Appearance ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Molar Ratio ◽  
Drug Release Study ◽  
Release Study

Objective: Ivabradine hydrochloride (IH), a benzazepine derivative used to treat cardiovascular disease angina pectoris. In this study IH-loaded novel carrier systems transfersomes (TFs) and conventional liposomes (CLs) were developed and compared for their efficacy to enhance the stability of drugs from degradation. Methods: TFs formulations (TF-1, TF-2 and TF-3) were prepared by using different biocompatible surfactants; tween-80 (TW), span-80(S) and sodium deoxycholate (SC) in the concentration ratio of 15 parts with 85 parts of soy phosphatidylcholine as phospholipid by thin-film hydration method. These vesicles were compared with CLs formulation (L-1) prepared in 7:3 molar ratio of soy phosphatidylcholine: cholesterol by following the same method. These vesicles were compared for physical appearance, vesicle shape, and size, percentage drug entrapment efficiency (%DEE), deformability index (DI), in vitro percentage cumulative drug release study, and physical stability studies. The chosen optimized novel carriers were observed under scanning electron microscopy. Results: The compared data demonstrated that the physical appearance for all vesicles was turbid and had a spherical shape. The size distribution was in the range of 129.0 nm to 273.5 nm in vesicles. The %DEE (79.0±0.94) and DI (35.0±1.9) was found maximum in TF-1 formulation that was 2.3 times higher than L-1 formulation. The in vitro percentage cumulative drug release study followed second-order polynomial kinetics that was 2.0 times higher than L-1and 2.9 times higher than the plain drug in 30 min (90.4±0.06%) from TF-1. The vesicles were found to be stable at refrigeration conditions. Conclusion: Thus, amongst of all vesicles TW loaded TFs (TF-1) was chosen as an excellent novel vesicular carrier for hydrophilic drugs due to its higher deformability behavior than CLs that protects the certain drugs from biodegradation and provides stability.

Oleanen Induces Apoptosis of Cervical Cancer Cells by Up-Regulation of Bim

2012 ◽  
Vol 22 (1) ◽  
pp. 38-42 ◽  
Author(s):  
Ningyue Gan ◽  
Gang Chen ◽  
Weijiang Zhang ◽  
Jianwei Zhou
Keyword(s):  
Cervical Cancer ◽  
Antitumor Activity ◽  
Hela Cells ◽  
Inhibitory Effect ◽  
Caspase 9 ◽  
Apoptosis Pathway ◽  
Cervical Cancer Cells ◽  
Caspase 6 ◽  
Apoptotic Pathways

ObjectivePlants belonging to the genus Celastrus exhibit antitumor activity and the ability to reverse multidrug resistance in tumor cells; however, it remains unclear whether the compound oleanen from Celastrus hypoleucus also exhibits antitumor activity. The objective of this study was to explore the inhibitory effect of 12-oleanene-3β, 6α-diol (oleanen) on the proliferation of cervical cancer HeLa cells in vitro, as well as its relative mechanism.MethodsHeLa cells were treated with different concentrations of oleanen for different times. Cell proliferation was determined by 3-(4,5)-dimethylthiahiazo (-z-y1)-3,5-di-phenytetrazoliumromide assay. Cell apoptosis was evaluated by flow cytometry and caspases activities assay. The expression of several proapoptotic proteins belonging to the Bcl-2 family, such as Bax, Bim, and Bad, was detected by Western blot.ResultsOleanen mainly inhibited the proliferation of HeLa cells at the G0 to G1 and G2 to M phases, and the IC50 of oleanen for cells was significantly higher at 24 hours compared to 48 hours (17.45 ± 3.71 vs 9.02 ± 0.83 μg/mL, respectively; P < 0.05). The significant increase in activity of caspase 3/7, caspase 6 in oleanen-treated HeLa cells indicated that oleanen promoted the apoptosis of HeLa cells. The activity of caspase 9 representing the endogenous apoptotic pathways also increased obviously in oleanen treatment. Furthermore, the increase in the expression of Bim was the most significant among the Bcl-2 family after oleanen treatment.ConclusionOleanen up-regulates the expression of Bim and other proapoptotic molecules to activate the endogenous apoptosis pathway, thus promoting apoptosis and inhibiting proliferation of human cervical cancer HeLa cells in vitro.

scholarly journals Hydroxyapatite/nifuroxazide conjugate: Characterization, drug release and antimicrobial activity

2021 ◽  
pp. 40-40
Author(s):  
Zeljko Radovanovic ◽  
Katarina Mihajlovski ◽  
Lidija Radovanovic ◽  
Djordje Janackovic ◽  
Rada Petrovic
Keyword(s):  
Drug Release ◽  
Raw Materials ◽  
Drug Carrier ◽  
In Vitro Study ◽  
Inhibitory Effect ◽  
Antibacterial Drug ◽  
Stomach Acid ◽  
Poorly Soluble ◽  
Good Biocompatibility

Synthetic hydroxyapatite (Ca10(PO4)6(OH)2, HAp) is very similar to the inorganic part of the bones and teeth of mammals. It is a well-known biomaterial with good biocompatibility, osteoconductivity and bioactivity. Nifuroxazide (C12H9N3O5, NFX) is a broad-spectrum antibacterial drug and poorly soluble in water. In order to increase the solubility of NFX, nanosized HAp powder and raw NFX drug were mixed giving, as a result, HAp/NFX conjugate. Characterization of the raw materials and the obtained conjugate confirmed the integration of NFX on the HAp surface. The in vitro study of drug release in simulated stomach acid and intestinal fluid showed a much faster release of NFX from HAp surface than those of raw drug. HAp/NFX conjugate showed an excellent inhibitory effect against Gram-positive bacterium Staphylococcus aureus, Gram-negative bacterium Escherichia coli and yeast Candida albicans, proving the nanosized HAp powder as a promising drug carrier.

scholarly journals Human natural killer cells can inhibit clonogenic growth of fresh leukemic cells

Blood ◽  
1983 ◽  
Vol 61 (3) ◽  
pp. 596-599
Author(s):  
M Beran ◽  
M Hansson ◽  
R Kiessling
Keyword(s):  
Nk Cells ◽  
Natural Killer ◽  
Nk Cell ◽  
Colony Growth ◽  
Inhibitory Effect ◽  
Leukemic Cells ◽  
Target Cells ◽  
Human Natural Killer Cells ◽  
Release Assay

The effect of allogenic human natural killer (NK) cells on fresh leukemic cells from three patients was investigated. The low levels of leukemic target cell lysis in the conventional 51Cr-release assay contrasted with a pronounced inhibitory effect on the colony growth of the clonogeneic leukemic target cells (L-CFC). The ability of allogeneic lymphocytes to inhibit L-CFC increased if they were pretreated with interferon (IFN), which also increased their NK activity, monitored in parallel cytotoxicity assay, against K562. Furthermore, cell separation procedures, based on differences in density among nonadherent lymphocytes, revealed that only NK cell containing fractions were inhibitory. We have also compared the susceptibility to NK-mediated L-CFC inhibition of IFN pretreated leukemic target cells with that of nontreated target cells. As in the case of NK lysis in general, this pretreatment of target cells abolished the presumably NK-mediated L-CFC inhibition. In conclusion, these data provide the first indication that NK cells can inhibit the in vitro growth of fresh clonogenic leukemia cells from patients with nonlymphocytic leukemia. The identity of NK cells as effector is strongly suggested by Percoll separation and responsiveness to interferon; the final proof awaits more sophisticated purification of these cells.

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