Acoustic Cluster Therapy (ACT®) enhances accumulation of polymeric micelles in the murine brain

In the case of solubility limited absorption, creating supersaturation in the GI fluid is very critical as supersaturation may provide great improvement of oral absorption. The techniques to create the so-called supersaturation in the GI fluid include microemulsions, emulsions, liposomes, complexations, polymeric micelles, and conventional micelles. Ciprofloxacin was chosen because it is practically insoluble in water; hence its salt form is used commercially, which is soluble in water. The objective of the present investigation was to enhance the solubility of Ciprofloxacin by formulating it into microemulsion system. For this purpose, initially, surfactant and cosurfactant were selected based on their HLB value, followed by pseudo-ternary phase diagrams to identify the microemulsion existing zone. Different formulations were developed and evaluated for pH, conductivity, in vitro release and stability. Solubility study was performed for optimized formulation. The pH of the designed formulations varied from 6.02-7.04. This was ideal and near blood pH 7.4. Conductivity data indicated that the microemulsion was of the o/w type. In vitro release of optimized formulation(FM3) was 95.2% as compared to pure drug 46.61% after 90 min and marketed product(salt form) 93.9%. Hence, by formulating into microemulsion, the solubility of ciprofloxacin is significantly enhanced.

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Preclinical Molecular Imaging of the Translocator Protein (TSPO) in a Metastases Model Based on Breast Cancer Xenografts Propagated in the Murine Brain

Current Molecular Medicine ◽

10.2174/1566524011207040458 ◽

2012 ◽

Vol 12 (4) ◽

pp. 458-466

Author(s):

Shelby K. Wyatt ◽

H. Charles Manning ◽

Mingfeng Bai ◽

Moneeb Ehtesham ◽

Khubaib Y. Mapara ◽

...

Keyword(s):

Breast Cancer ◽

Molecular Imaging ◽

Translocator Protein ◽

Model Based ◽

Murine Brain ◽

Breast Cancer Xenografts

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Tissue Distribution and Systemic Toxicity Evaluation of Raloxifene Targeted Polymeric Micelles of Poly (Styrene-Maleic Acid)-Poly (Amide- Ether-Ester-Imide)-Poly (Ethylene Glycol) Loaded With Docetaxel in Breast Cancer Bearing Mice

Recent Patents on Anti-Cancer Drug Discovery ◽

10.2174/1574892814666190919163731 ◽

2019 ◽

Vol 14 (3) ◽

pp. 280-291 ◽

Cited By ~ 1

Author(s):

Jaleh Varshosaz ◽

Farshid Hassanzadeh ◽

Batool Hashemi-Beni ◽

Mohsen Minaiyan ◽

Saeedeh Enteshari

Keyword(s):

Side Effects ◽

Antitumor Activity ◽

Ethylene Glycol ◽

Tissue Distribution ◽

Tumor Cells ◽

Maleic Acid ◽

Polymeric Micelles ◽

Poly Ethylene Glycol ◽

Poly Ethylene ◽

Ether Ester

Background: Due to the low water solubility of Docetaxel (DTX), it is formulated with ethanol and Tween 80 with lots of side effects. For this reason, special attention has been paid to formulate it in new drug nano-carriers. Objective: The goal of this study was to evaluate the safety, antitumor activity and tissue distribution of the novel synthesized Raloxifene (RA) targeted polymeric micelles. Methods: DTX-loaded RA-targeted polymeric micelles composed of poly(styrene-maleic acid)- poly(amide-ether-ester-imide)-poly(ethylene glycol) (SMA-PAEE-PEG) were prepared and their antitumor activity was studied in MC4-L2 tumor-bearing mice compared with non-targeted micelles and free DTX. Safety of the micelles was studied by Hematoxylin and Eosin (H&E) staining of tumors and major organs of the mice. The drug accumulation in the tumor and major organs was measured by HPLC method. Results: The results showed better tumor growth inhibition and increased survival of mice treated with DTX-loaded in targeted micelles compared to the non-targeted micelles and free DTX. Histopathological studies, H&E staining of tumors and immunohistochemical examination showed the potential of DTX-loaded RA-targeted micelles to inhibit tumor cells proliferation. The higher accumulation of the DTX in the tumor tissue after injection of the micelles compared to the free DTX may indicate the higher uptake of the targeted micelles by the G-Protein-Coupled Estrogen Receptors (GPER). Conclusion: The results indicate that RA-conjugated polymeric micelles may be a strong and effective drug delivery system for DTX therapy and uptake of the drug into tumor cells, and overcome the disadvantages and side effects of conventional DTX.

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Recent Nanocarrier Approaches for Targeted Drug Delivery in Cancer Therapy

Current Molecular Pharmacology ◽

10.2174/1874467213666200730114943 ◽

2020 ◽

Vol 13 ◽

Author(s):

Rohit Bhatia ◽

Amit Sharma ◽

Raj Kumar Narang ◽

Ravindra K. Rawal

Keyword(s):

Drug Delivery ◽

Polymeric Micelles ◽

Mesoporous Silica Nanoparticles ◽

Treatment Strategies ◽

Human Beings ◽

The Past ◽

Organ Systems ◽

Metal Organic ◽

Continuous Progress ◽

Chemotherapeutic Treatment

: Cancer is one of the most serious health concerns in 21st century whose prevalence is beyond boundaries and can affect any organ of human beings. The conventional chemotherapeutic treatment strategies lack specificity to tumours and are associated with toxic effects on immune system and other organ systems. In the past decades, there has been a continuous progress in the development of smart nanocarrier systems for target specific delivery of drugs against variety of tumours including intracellular gene-specific targeting. These nanocarriers are able to recognize the tumour cells and deliver the therapeutic agent in fixed proportions causing no or very less harm to healthy cells. Nanosystems have modified physicochemical properties, improved bioavailability and long retention in blood which enhances their potency. A huge number of nanocarrier based formulations have been developed and are in clinical trials. Nanocarrier systems include polymeric micelles, liposomes, dendrimers, carbon nanotubes, gold nanoparticles, etc. Recent advancements in nanocarrier systems include mesoporous silica nanoparticles (MSNs), metal organic frame works and quantum dots. In the present review, various nanocarrier based drug delivery systems along with their applications in the management of cancer have been described with special emphasis on MSNs.

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