scholarly journals Pemanfaatan Ekstrak Daun Mangrove (Rhizophora mucronata sp.) dengan Variasi Pelarut Sebagai Bahan Aktif Sediaan Farmasi Terapi Anti Kanker

2017 ◽  
Vol 4 (2) ◽  
pp. 68 ◽  
Author(s):  
Anita Ratna Faoziyah ◽  
Wahyu Kurniawan
Keyword(s):  
Drug Loading ◽  
Economic Value ◽  
Tween 80 ◽  
Second Phase ◽  
Rhizophora Mucronata ◽  
Anti Cancer ◽  
Young Leaves ◽  
Research Goal ◽  
Emulsion Formulation ◽  
Nano Emulsion

This research was done to study mangrove leaves (Rhizophora mucronata sp.) utilization in the Cilacap regency brackish waters. The research goal is to make nano emulsion from mangrove plants as an alternative to increase the economic value of mangrove. This research method has 2 phases. In the first phase, mangrove leaves was extracted using various solvent. In the second phase mangrove leaves extract was formulated as nano emulsion as anti-cancer treatment along as an alternative to increase mangrove leaves economic value. Extraction results of mangrove leaves using various solvent such as hexane, ethyl acetate and ethanol show that using ethanol p.a solvent with the young leaves of mangrove giving the highest amount extract as much as 18.24%. Mangrove leaves extract nano emulsion can be prepared using Self-Nano Emulsifying Drug Delivery System (SNEDDS) technique. The SNEDDS technique nano emulsion formulation started with 14 formulas. The best formula from this study was using Tween 80 : PEG 400 : Fish Oil as much as 6 ml: 1 ml: 1 ml dosage ratio. Using the best formula, it was added with 5 mg of mangrove leaves extract. The result test of Drug Loading, calculation of Emulsification Time and Dissolution test show that mangrove leaves extract has the potential to be used as an active substance anti-cancer on nano emulsion manufacturing.

Stereocomplexation Assisted Assembly of Poly(γ-glutamic Acid)-graft-polylactide Nano-micelles and Their Efficacy as Anticancer Drug Carrier

2018 ◽  
Vol 18 (2) ◽  
pp. 302-311
Author(s):  
Shulin Dai ◽  
Yucheng Feng ◽  
Shuyi Li ◽  
Yuxiao Chen ◽  
Meiqing Liu ◽  
...  
Keyword(s):  
Glutamic Acid ◽  
Drug Carrier ◽  
Drug Loading ◽  
Drug Carriers ◽  
Cancer Drug ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
Anti Cancer ◽  
Physical Interactions

Background: Micelles as drug carriers are characterized by their inherent instability due to the weak physical interactions that facilitate the self-assembly of amphiphilic block copolymers. As one of the strong physical interactions, the stereocomplexation between the equal molar of enantiomeric polylactides, i.e., the poly(L-lactide) (PLLA) and poly(D-lactide) (PDLA), may be harnessed to obtain micelles with enhanced stability and drug loading capacity and consequent sustained release. </P><P> Aims/Methods: In this paper, stereocomplexed micelles gama-PGA-g-PLA micelles) were fabricated from the stereocomplexation between poly(gama-glutamic acid)-graft-PLLA gama-PGA-g-PLA) and poly(gamaglutamic acid)-graft-PDLA gama-PGA-g-PLA). These stereocomplexed micelles exhibited a lower CMC than the corresponding enantiomeric micelles. Result: Furthermore, they showed higher drug loading content and drug loading efficiency in addition to more sustained drug release profile in vitro. In vivo imaging confirmed that the DiR-encapsulated stereocomplexed gama-PGA-g-PLA micelles can deliver anti-cancer drug to tumors with enhanced tissue penetration. Overall, gama-PGA-g-PLA micelles exhibited greater anti-cancer effects as compared with the free drug and the stereocomplexation may be a promising strategy for fabrication of anti-cancer drug carriers with significantly enhanced efficacy.

scholarly journals Preparation of Catechin Nanoemulsion from Oolong Tea Leaf Waste and Its Inhibition of Prostate Cancer Cells DU-145 and Tumors in Mice

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3260
Author(s):  
Yu-Hsiang Lin ◽  
Chi-Chung Wang ◽  
Ying-Hung Lin ◽  
Bing-Huei Chen
Keyword(s):  
Prostate Cancer ◽  
Cancer Cells ◽  
Tumor Volume ◽  
Tween 80 ◽  
Prostate Cancer Cells ◽  
Caspase 9 ◽  
Oolong Tea ◽  
Induced Tumors ◽  
Anti Cancer ◽  
Tea Leaf

Anti-cancer activity of catechin nanoemulsions prepared from Oolong tea leaf waste was studied on prostate cancer cells DU-145 and DU-145-induced tumors in mice. Catechin nanoemulsions composed of lecithin, Tween-80 and water in an appropriate proportion was prepared with high stability, particle size of 11.3 nm, zeta potential of −67.2 mV and encapsulation efficiency of 83.4%. Catechin nanoemulsions were more effective than extracts in inhibiting DU-145 cell growth, with the IC50 being 13.52 and 214.6 μg/mL, respectively, after 48 h incubation. Furthermore, both catechin nanoemulsions and extracts could raise caspase-8, caspase-9 and caspase-3 activities for DU-145 cell apoptosis, arresting the cell cycle at S and G2/M phases. Compared to control, catechin nanoemulsion at 20 μg/mL and paclitaxel at 10 μg/mL were the most effective in reducing tumor volume by 41.3% and 52.5% and tumor weight by 77.5% and 90.6% in mice, respectively, through a decrease in EGF and VEGF levels in serum.

scholarly journals Development, Characterization, and Immunomodulatory Evaluation of Carvacrol-loaded Nanoemulsion

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3899
Author(s):  
Amanda Gabrielle Barros Dantas ◽  
Rafael Limongi de de Souza ◽  
Anderson Rodrigues de de Almeida ◽  
Francisco Humberto Xavier Xavier Júnior ◽  
Maira Galdino da Rocha Pitta ◽  
...  
Keyword(s):  
Drug Loading ◽  
Tween 80 ◽  
Immunomodulatory Activity ◽  
Peripheral Blood Mononuclear ◽  
Pbmc Culture ◽  
Phase Medium ◽  
Therapeutic Properties ◽  
Ifn Γ ◽  
Immunomodulatory Action ◽  
Culture Supernatants

Carvacrol (CV) is an essential oil with numerous therapeutic properties, including immunomodulatory activity. However, this effect has not been studied in nanoemulsion systems. The objective of this study was to develop an innovative carvacrol-loaded nanoemulsion (CVNE) for immunomodulatory action. The developed CVNE comprised of 5% w/w oily phase (medium chain triglycerides + CV), 2% w/w surfactants (Tween 80®/Span 80®), and 93% w/w water, and was produced by ultrasonication. Dynamic light scattering over 90 days was used to characterize CVNE. Cytotoxic activity and quantification of cytokines were evaluated in peripheral blood mononuclear cell (PBMC) culture supernatants. CVNE achieved a drug loading of 4.29 mg/mL, droplet size of 165.70 ± 0.46 nm, polydispersity index of 0.14 ± 0.03, zeta potential of −10.25 ± 0.52 mV, and good stability for 90 days. CVNE showed no cytotoxicity at concentrations up to 200 µM in PBMCs. CV diminished the production of IL-2 in the PBMC supernatant. However, CVNE reduced the levels of the pro-inflammatory cytokines IL-2, IL-17, and IFN-γ at 50 µM. In conclusion, a stable CVNE was produced, which improved the CV immunomodulatory activity in PBMCs.

Simultaneous Incorporation of 5-Fluorouracil and Leucovorin into Chitosan Nanoparticle as Drug Carrier and Its Characterization

2010 ◽  
Vol 654-656 ◽  
pp. 2265-2268
Author(s):  
Pu Wang Li ◽  
Yi Chao Wang ◽  
Zheng Peng ◽  
Ling Xue Kong
Keyword(s):  
Particle Size ◽  
Strong Interaction ◽  
Encapsulation Efficiency ◽  
Drug Carrier ◽  
Drug Loading ◽  
Anti Cancer ◽  
Chitosan Nanoparticle ◽  
Combined Drugs ◽  
Drug Encapsulation Efficiency ◽  
Interaction Between Drugs

A combined drug loaded system containing two most common anti-cancer drugs 5-fluorouracil (5-FU) and leucovorin (LV) was designed and prepared by ion crosslinking technology. The resulted nanoparticles are spherical in shape, and the particle size becomes larger when drug combination are loaded. Efficient drug encapsulation efficiency (EE) and drug loading (LC) are obtained due to the strong interaction between drugs and polymer. The combined drugs are distributed in the particles in amorpholous state which are demonstrated by the XRD results.

scholarly journals Study of the Activity of 3-benzyl-5-(4-chloro-arylazo)-4-thioxo-imidazolidin-2-one against Schistosomiasis Mansoni in Mice

2012 ◽  
Vol 2012 ◽  
pp. 1-8 ◽  
Author(s):  
Andréa Cristina Apolinário da Silva ◽  
Juliana Kelle de Andrade Lemoine Neves ◽  
João Inácio Irmão ◽  
Vláudia Maria Assis Costa ◽  
Valdênia Maria Oliveira Souza ◽  
...  
Keyword(s):  
Specific Antigen ◽  
Tween 80 ◽  
Histopathological Analysis ◽  
Second Phase ◽  
No Production ◽  
Potential Candidate ◽  
Treatment Regimens ◽  
Morphological Aspects ◽  
Oil Water

Previous studies conducted with the imidazolidinic derivative 3-benzyl-5-(4-chloro-arylazo)-4-thioxo-imidazolidin-2-one (LPSF-PT05) show outstanding activity against adultSchistosoma mansoniwormsin vitro. In the first phase of this study,S. mansoni-infected mice were treated, orally, with 100 mg/Kg of the LPSF-PT05 in three formulations: Tween 80 and saline solution, oil/water (70 : 30) emulsion, and solid dispersion with polyethylene glycol (PEG). In the second phase, three other doses of the LPSF-PT05 in PEG were tested: 3, 10, 30 mg/kg. These treatment regimens significantly reduced the number of recovered worms due to increases in the solubility of the compound in this formulation; the greatest reduction (70.5%) was observed at the dose of 100 mg/kg. There was no changes in the pattern of mature egg compared to immature eggs; however there was a significant increase in the number of dead eggs. Histopathological analysis of liver tissue showed changes in morphological aspects of the hepatic parenchyma with decrease exudative-productive hepatic granuloma stages, although we found no significant differences in IFN-γ, IL-4, IL-10, or NO production in response to the specific antigen SEA. The results show the derivative LPSF-PT05 to be a potential candidate in the etiological treatment of schistosomiasis with a possible dampening effect of the granulomatous process.

scholarly journals Formulation, Development and Evaluation of Ibuprofen Loaded Nano-transferosomal Gel for the Treatment of Psoriasis

2019 ◽  
pp. 1-8
Author(s):  
Marwa H. Abdallah ◽  
Amr S. Abu Lila ◽  
Md. Khalid Anwer ◽  
El-Sayed Khafagy ◽  
Muqtader Mohammad ◽  
...  
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Vesicle Size

The present work was aimed to develop a transferosomal gel of ibuprofen (IBU) for the amelioration of psoriasis like inflammation. Three formulation of IBU loaded transferosomes (TFs1-TFs3) were prepared using different proportions of lipid (phospholipon 90H) and surfactant (tween 80) and further evaluated for vesicle size, zeta potential (ZP), entrapment efficiency and in vitro drug release. The IBU loaded transferosomes (TFs2) was optimized with vesicle size (217±8.4 nm), PDI (0.102), ZP (-31.5±4.3 mV), entrapment efficiency (88.4±6.9%) and drug loading (44.2±2.9%). Further, the optimized IBU loaded transferosomes (TFs2) was incorporated into 1% carbopol 934 gel base and characterized for homogeneity, extrudability, viscosity and drug content. The in vivo pharmacodynamic study of gel exhibited reduction in psoriasis like inflammation in mice. The ibuprofen loaded transferosomal gel was successfully developed and has shown the potential to be a new therapy against psoriasis like inflammation.

Surfactant-Based Anhydrous Nano Carrier System for Poorly Aqueous Soluble Anti-Cancer Drugs

2021 ◽  
pp. 413-432
Author(s):  
Shekhar Verma ◽  
Nagendra Chandrawanshi ◽  
Vishal Jain
Keyword(s):  
Controlled Release ◽  
Primary Objective ◽  
Water Soluble ◽  
Cancer Drug ◽  
Cancer Drugs ◽  
Carrier System ◽  
Anti Cancer ◽  
New Chemical Entities ◽  
Poorly Water Soluble ◽  
Nano Emulsion

Around 40% of new chemical entities and drugs are lipophilic or poor aqueous soluble in nature. Among them many anti-cancer drugs are also consist lipophilic properties. Available poorly water soluble anti-cancer drugs are paclitaxel, etoposide, and docetaxel. To get better stability of those anti-cancer drug via encapsulation and searching suitable carrier system for the controlled release, design and development requires of anhydrous nano carrier system. However, to deliver and entrapment of these kind of anti-cancer drugs are very essential with avoidance of water free preparation to get suitable controlled release application and achieve targeting site. The primary objective of proposed chapter is to develop and design novel stable anhydrous or non-aqueous nano emulsion carrier system and provide suitable carrier system for poorly aqueous soluble anti-cancer drugs. Another important aim is to design and develop better stabilizing agent by combining different type of surfactant, co-surfactant, and co-solvent.

Co-delivery of dual chemo-drugs with precisely controlled, high drug loading polymeric micelles for synergistic anti-cancer therapy

2020 ◽  
Vol 8 (3) ◽  
pp. 949-959 ◽  
Author(s):  
Yuchen Wu ◽  
Shixian Lv ◽  
Yongjuan Li ◽  
Hua He ◽  
Yong Ji ◽  
...  
Keyword(s):  
Cancer Therapy ◽  
Polymeric Micelles ◽  
Drug Loading ◽  
High Drug ◽  
Delivery Strategy ◽  
Anti Cancer ◽  
High Drug Loading

The introduction of donor-receptor coordination between micelles and drug payloads provides a precise co-delivery strategy for two different chemo-drugs with high drug loading and ROS responsiveness.

scholarly journals Preparation and Characterization of PEG-PLA Genistein Micelles Using a Modified Emulsion-Evaporation Method

2020 ◽  
Vol 2020 ◽  
pp. 1-15
Author(s):  
Qiuchen Cheng ◽  
Wen Qin ◽  
Yanhong Yu ◽  
Guojian Li ◽  
Jizhou Wu ◽  
...  
Keyword(s):  
Smooth Muscle Actin ◽  
Drug Loading ◽  
In Vitro Release ◽  
Tween 80 ◽  
Original Method ◽  
Scanning Calorimetry ◽  
Experimental Conditions ◽  
Evaporation Method ◽  
Genistein Treatment

The objective of this study is to improve the bioavailability of genistein by encapsulation with polyethylene glycol-polylactic acid (PEG-PLA) copolymers. Genistein micelles (GMs) prepared using a modified emulsion-evaporation method were more stable than those made with the original method. The effect of polyvinyl alcohol, Tween 80, sonication time, PEG-PLA/genistein ratio, and organic phase (acetone)/H2O ratio on the size, polydispersity index, encapsulation efficiency, and drug loading efficiency of GMs was investigated. GMs were obtained and characterized under optimal experimental conditions. For long-term storage, GMs were lyophilized by freeze drying with trehalose to produce genistein lyophilized powder (GLP). The analysis of GLP by Fourier-transform infrared spectroscopy and differential scanning calorimetry showed that genistein was successfully incorporated into the micellar structure. In vitro release experiments revealed that the incorporation of genistein into PEG-PLA copolymers significantly improved its solubility and bioavailability. GLP was more potent in inhibiting the proliferation of HSC-T6 cells than genistein. Treatment with GLP at 10–20 μg/mL for 48 h significantly inhibited the protein expression of α-smooth muscle actin and collagen I in HSC-T6 cells compared with the control. These data demonstrated that the improved solubility and bioavailability of genistein in the form of GLP enhanced its antifibrotic effect in vitro.

scholarly journals Nanoparticles based on retinoic acid caped with ferrocenium: a novel synthesized targetable nanoparticle both with anti-cancer effect and drug loading capacity

RSC Advances ◽  
2019 ◽  
Vol 9 (28) ◽  
pp. 16208-16214 ◽  
Author(s):  
Yibo Wang ◽  
Bin Zhao ◽  
Lu Wang ◽  
Wenhuan Bu ◽  
Shuwei Liu ◽  
...  
Keyword(s):  
Retinoic Acid ◽  
Drug Loading ◽  
Cancer Drug ◽  
Loading Capacity ◽  
Anti Cancer

A retinoic acid nanoparticle with the ability of carrying a second anti-cancer drug, taxol, was developed. The anti-cancer nanoparticles were shown to have a better application prospect than that of RA or taxol alone.

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