scholarly journals Umbelliferone Decorated Water‐soluble Zinc(II) Phthalocyanines – In Vitro Phototoxic Antimicrobial Anti‐cancer Agents

2021 ◽  
Author(s):  
Andrea Sowa ◽  
Alexander Höing ◽  
Ulrich Dobrindt ◽  
Shirley K. Knauer ◽  
Anzhela Galstyan ◽  
...  
Keyword(s):  
Water Soluble ◽  
Anti Cancer ◽  
Soluble Zinc

scholarly journals Efflux Inhibitor Bicalutamide Increases Oral Bioavailability of the Poorly Soluble Efflux Substrate Docetaxel in Co-Amorphous Anti-Cancer Combination Therapy

Molecules ◽  
2019 ◽  
Vol 24 (2) ◽  
pp. 266 ◽  
Author(s):  
Adam Bohr ◽  
Thais Nascimento ◽  
Necati Harmankaya ◽  
Johan Weisser ◽  
Yingya Wang ◽  
...  
Keyword(s):  
Efflux Pump ◽  
Water Soluble ◽  
Oral Dosage ◽  
In Vitro Dissolution ◽  
Molar Ratio ◽  
Cancer Drugs ◽  
Efflux Pump Inhibitor ◽  
Anti Cancer ◽  
Amorphous Formulation

Many anti-cancer drugs are difficult to formulate into an oral dosage form because they are both poorly water-soluble and show poor permeability, the latter often as a result of being an intestinal efflux pump substrate. To obtain a more water-soluble formulation, one can take advantage of the higher solubility of the amorphous form of a given drug, whereas to increase permeability, one can make use of an efflux pump inhibitor. In this study, a combination of these two strategies was investigated using the co-amorphous approach, forming an amorphous mixture of two anti-cancer drugs, docetaxel (DTX) and bicalutamide (BIC). The efflux substrate, DTX, was combined with the efflux inhibitor, BIC, and prepared as a single phase co-amorphous mixture at a 1:1 molar ratio using vibrational ball milling. The co-amorphous formulation was tested in vitro and in vivo for its dissolution kinetics, supersaturation properties and pharmacokinetics in rats. The co-amorphous formulation showed a faster in vitro dissolution of both drugs compared to the control groups, but only DTX showed supersaturation (1.9 fold) compared to its equilibrium solubility. The findings for the co-amorphous formulation were in agreement with the pharmacokinetics data, showing a quicker onset in plasma concentration as well as a higher bioavailability for both DTX (15-fold) and BIC (3-fold) compared to the crystalline drugs alone. Furthermore, the co-amorphous formulation remained physically stable over 1.5 years at 4 °C under dry conditions.

scholarly journals Synthesis and anti-cancer activities of a water soluble gold(III) porphyrin

2015 ◽  
Vol 19 (01-03) ◽  
pp. 398-403 ◽  
Author(s):  
Aaron D. Lammer ◽  
Melissa E. Cook ◽  
Jonathan L. Sessler
Keyword(s):  
Anticancer Agents ◽  
Ovarian Cancer Cell ◽  
Ovarian Cancer Cell Line ◽  
Aqueous Media ◽  
Cancer Cell Line ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Physiological Conditions ◽  
Anti Cancer

Gold(III) compounds continue to be explored for their potential utility as anticancer agents. A recognized limitation is the reactivity of gold(III), which is typically reduced to the more labile gold(I) state under physiological conditions. The use of porphyrins can overcome this problem. However, to date the stabilization provided by the use a strongly chelating porphyrin is offset by the poor solubility of the resulting complex in aqueous media. In this work, we describe the synthesis and in vitro anti-cancer activity of a gold(III)porphyrin complex with relatively good aqueous solubility. As judged from standard antiproliferation assays, this complex displays an IC50 of 9 μM for the A2780 human ovarian cancer cell line. This is a higher level of potency than displayed by two related control systems.

scholarly journals Phycocyanin from Arthrospira platensis as Potential Anti-Cancer Drug: Review of In Vitro and In Vivo Studies

Life ◽  
2021 ◽  
Vol 11 (2) ◽  
pp. 91
Author(s):  
Steffen Braune ◽  
Anne Krüger-Genge ◽  
Sarah Kammerer ◽  
Friedrich Jung ◽  
Jan-Heiner Küpper
Keyword(s):  
Molecular Mechanisms ◽  
Arthrospira Platensis ◽  
Water Soluble ◽  
In Vivo Studies ◽  
Cancer Drug ◽  
Cancer Therapies ◽  
Natural Substances ◽  
Anti Cancer

The application of cytostatic drugs or natural substances to inhibit cancer growth and progression is an important and evolving subject of cancer research. There has been a surge of interest in marine bioresources, particularly algae, as well as cyanobacteria and their bioactive ingredients. Dried biomass products of Arthrospira and Chlorella have been categorized as “generally recognized as safe” (GRAS) by the US Food and Drug Administration (FDA). Of particular importance is an ingredient of Arthrospira: phycocyanin, a blue-red fluorescent, water-soluble and non-toxic biliprotein pigment. It is reported to be the main active ingredient of Arthrospira and was shown to have therapeutic properties, including anti-oxidant, anti-inflammatory, immune-modulatory and anti-cancer activities. In the present review, in vitro and in vivo data on the effects of phycocyanin on various tumor cells and on cells from healthy tissues are summarized. The existing knowledge of underlying molecular mechanisms, and strategies to improve the efficiency of potential phycocyanin-based anti-cancer therapies are discussed.

scholarly journals A COMPREHENSIVE REVIEW ON SUPERSATURABLE SELF-NANOEMULSIFYING DRUG DELIVERY SYSTEM

2021 ◽  
pp. 40-44
Author(s):  
MUTHADI RADHIKA REDDY ◽  
KUMAR SHIVA GUBBIYAPPA
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Water Soluble ◽  
In Vitro Tests ◽  
Drug Bioavailability ◽  
Advantages And Disadvantages ◽  
Anti Cancer

Lipid-based drug delivery systems are extensively reported in the literature for enhancing drug solubility, permeability, and bioavailability. Self-nanoemulsifying drug delivery systems (SNEDDS) are a superior strategy for enhancing solubility and bioavailability of poorly water-soluble compounds and the most prevailing and commercially viable oil-based approach for drugs that exhibit low dissolution rate and inadequate absorption. However, these formulations have few limitations that include in vivo drug precipitation, inferior in vitro in vivo correlation owing to unavailability of in vitro tests, handling issues of liquid formulation, and physicochemical instability of drugs. These limitations are overcome by potential systems such as supersaturable SNEDDS (S-SNEDDS) which are prepared by addition of precipitation inhibitors into formulated SNEDDS to maintain drug supersaturation post dispersion in gastrointestinal tract. These systems improve drug bioavailability and reduce the inconsistency of exposure. In addition, these formulations also help to overcome the drawbacks of liquid and capsule dosage forms. The S-SNEDDS provides an effective approach for improving the dissolution and bioavailability of anti-cancer agents. In this article, an attempt was made to present an overview of SNEDDS, S-SNEDDS, their mechanism, formulation excipients, recent advancements, advantages, and disadvantages of SNEDDS formulations. The article also focuses on reviewing the application of S-SNEDDS in enhancing the solubility and bioavailability of anti-cancer drugs in cancer therapy.

Curcumin Nanoemulsion: Evaluation of Stability and Anti-Cancer Activity In Vitro

2020 ◽  
Vol 64 ◽  
pp. 21-37
Author(s):  
Thanh Binh Nguyen ◽  
Thi Mai Huong Nguyen ◽  
Thi Thu Huong Le ◽  
Thi Thuy Phan ◽  
Trong Tinh Nguyen ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Cell Lines ◽  
Water Solubility ◽  
Oral Absorption ◽  
Curcuma Longa ◽  
Water Soluble ◽  
Therapeutic Drug ◽  
Cytotoxic Activities ◽  
Anti Cancer

Curcumin is a phytochemical compound extracted from the rhizomes of the plant Curcuma longa and shows intrinsic anti-cancer properties. Its medical application remains limited due to its extremely low water solubility and bioavailability. Addressing this problem, drug delivery systems based on nano-scale technology have emerged. Among the advanced techniques, the self-nano-emulsifying drug delivery system (SNEDDS) has been considered as an ideal method to enhance the oral absorption and bioavailability of poorly water-soluble drugs. The objectives of present study are to prepare a formulation of nanoemulsion containing curcuminoids of natural origin, assess its micro properties, stabilities and evaluate the in vitro cytotoxic activity against some cancer cells using tetrazolium dye MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazo- lium bromide] (MTT assay). Measurement results showed that the curcumin nanoemulsion was successfully synthesized with typical mean droplet sizes from 9 to 11 nm, and revealed an excellent stability over time. Curcumin in a nanoemulsion was more stable than unencapsulated curcumin. In vitro experiments on cytotoxic activities against Hela, HepG2 and H460 cancer cell lines indicated that the prepared curcumin nanoemulsion effectively inhibited the growth of all three cell lines with IC50 values of 8.6 µM, 14.5 µM and 5.3 µM respectively. Results of this study suggest that curcumin nanoemulsion can be considered as novel and promising chemo-preventive and therapeutic drug in treatment of cancer, and it may supply some useful ideas in developing anticancer drugs for further in vivo studies.

Poly(2-methyl-2-oxazoline) conjugates with doxorubicin: From synthesis of high drug loading water-soluble constructs to in vitro anti-cancer properties

2020 ◽  
Vol 326 ◽  
pp. 53-62
Author(s):  
Ondrej Sedlacek ◽  
Alexandra Van Driessche ◽  
Annemiek Uvyn ◽  
Bruno G. De Geest ◽  
Richard Hoogenboom
Keyword(s):  
Drug Loading ◽  
Water Soluble ◽  
High Drug ◽  
Anti Cancer ◽  
High Drug Loading

Controlled Release of Metformin Hydrochloride I. In vitro Release from Physical Mixture Containing Xanthan Gum as Hydrophilic Rate Retarding Polymer

1970 ◽  
Vol 4 (1) ◽  
Author(s):  
Mashkura Ashrafi ◽  
Jakir Ahmed Chowdhury ◽  
Md Selim Reza
Keyword(s):  
Controlled Release ◽  
Xanthan Gum ◽  
In Vitro Release ◽  
Correlation Coefficients ◽  
High Ratio ◽  
Water Soluble ◽  
Metformin Hydrochloride ◽  
Model Drug ◽  
Very High

Capsules of different formulations were prepared by using a hydrophilic polymer, xanthan gum and a filler Ludipress. Metformin hydrochloride, which is an anti-diabetic agent, was used as a model drug here with the aim to formulate sustained release capsules. In the first 6 formulations, metformin hydrochloride and xanthan gum were used in different ratio. Later, Ludipress was added to the formulations in a percentage of 8% to 41%. The total procedure was carried out by physical mixing of the ingredients and filling in capsule shells of size ‘1’. As metformin hydrochloride is a highly water soluble drug, the dissolution test was done in 250 ml distilled water in a thermal shaker (Memmert) with a shaking speed of 50 rpm at 370C &plusmn 0.50C for 6 hours. After the dissolution, the data were treated with different kinetic models. The results found from the graphs and data show that the formulations follow the Higuchian release pattern as they showed correlation coefficients greater than 0.99 and the sustaining effect of the formulations was very high when the xanthan gum was used in a very high ratio with the drug. It was also investigated that the Ludipress extended the sustaining effect of the formulation to some extent. But after a certain period, Ludipress did not show any significant effect as the pores made by the xanthan gum network were already blocked. It is found here that when the metformin hydrochloride and the xanthan gum ratio was 1:1, showed a high percentage of drug release, i.e. 91.80% of drug was released after 6 hours. But With a xanthan gum and metformin hydrochloride ratio of 6:1, a very slow release of the drug was obtained. Only 66.68% of the drug was released after 6 hours. The percent loading in this case was 14%. Again, when Ludipress was used in high ratio, it was found to retard the release rate more prominently. Key words: Metformin Hydrochloride, Xanthan Gum, Controlled release capsule Dhaka Univ. J. Pharm. Sci. Vol.4(1) 2005 The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website

NGHIÊN CỨU ẢNH HƯỞNG CỦA CHITOSAN HOÀ TAN TRONG NƯỚC ĐẾN NẤM Colletotrichum musae D1 GÂY BỆNH THÁN THƯ TRÊN CHUỐI Ở ĐIỀU KIỆN IN VITRO

2016 ◽  
Vol 119 (5) ◽  
Author(s):  
Lê Thanh Long ◽  
Nguyễn Văn Toản ◽  
Nguyễn Văn Huế ◽  
Trang Sĩ Trung ◽  
Vũ Ngọc Bội
Keyword(s):  
Water Soluble ◽  
28S Rrna ◽  
Colletotrichum Musae

Chủng D1 phân lập từ các mẫu chuối có vết bệnh thán thư điển hình được sử dụng để nghiên cứu khả năng kháng nấm của chitosan hoà tan trong nước (Water-soluble chitosan_WSC) ở điều kiện in vitro. Kết quả phân tích trình tự gen mã hoá 28S rRNA của chủng D1 cho thấy tương đồng trình tự cao với các trình tự tương ứng của loài Colletotrichum musae và được ký hiệu là Colletotrichum musae D1. Kết quả các thí nghiệm đều cho thấy C. musae D1 rất nhạy cảm với WSC, hiệu lực ức chế tăng khi tăng nồng độ WSC xử lý ở điều kiện in vitro. Trên môi trường PDA, nồng độ 1,6% WSC ức chế hoàn toàn sự sinh trưởng của sợi nấm C. musae D1, nồng độ ức chế 50% (PIRG50) và nồng độ ức chế tối thiểu 90% (MIC90) tương ứng với nồng độ WSC 0,28% và 0,88%. Trong môi trường PDB, giá trị IC50 và MIC90 tương ứng là 0,11% và 0,43% và sự phát triển của sợi nấm C. musae D1 bị ức chế hoàn toàn ở nồng độ 0,8%. WSC không chỉ ức chế sự nảy mầm mà còn gây biến đổi bất thường bào tử nấm khi quan sát trên kính hiển vi.

Sign in / Sign up

Export Citation Format

Share Document