Development of 6-Thioguanine conjugated PLGA nanoparticles through thioester bond formation: Benefits of electrospray mediated drug encapsulation and sustained release in cancer therapeutic applications

2020 ◽  
Vol 114 ◽  
pp. 111029
Author(s):  
Manosree Chatterjee ◽  
Namita Jaiswal ◽  
Abhiram Hens ◽  
Nibedita Mahata ◽  
Nripen Chanda
Keyword(s):  
Sustained Release ◽  
Bond Formation ◽  
Plga Nanoparticles ◽  
Drug Encapsulation ◽  
Therapeutic Applications ◽  
Thioester Bond

scholarly journals Red Blood Cell Membrane-Camouflaged Tedizolid Phosphate-Loaded PLGA Nanoparticles for Bacterial-Infection Therapy

Pharmaceutics ◽  
2021 ◽  
Vol 13 (1) ◽  
pp. 99
Author(s):  
Xinyi Wu ◽  
Yichen Li ◽  
Faisal Raza ◽  
Xuerui Wang ◽  
Shulei Zhang ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Cell Membrane ◽  
Blood Cell ◽  
Sustained Release ◽  
Delivery System ◽  
Red Blood Cell ◽  
Multiple Drug Resistance ◽  
Plga Nanoparticles ◽  
Multiple Drug ◽  
Red Blood Cell Membrane

Multiple drug resistance (MDR) in bacterial infections is developed with the abuse of antibiotics, posing a severe threat to global health. Tedizolid phosphate (TR-701) is an efficient prodrug of tedizolid (TR-700) against gram-positive bacteria, including methicillin-sensitive staphylococcus aureus (MSSA) and methicillin-resistant staphylococcus aureus (MRSA). Herein, a novel drug delivery system: Red blood cell membrane (RBCM) coated TR-701-loaded polylactic acid-glycolic acid copolymer (PLGA) nanoparticles (RBCM-PLGA-TR-701NPs, RPTR-701Ns) was proposed. The RPTR-701Ns possessed a double-layer core-shell structure with 192.50 ± 5.85 nm in size, an average encapsulation efficiency of 36.63% and a 48 h-sustained release in vitro. Superior bio-compatibility was confirmed with red blood cells (RBCs) and HEK 293 cells. Due to the RBCM coating, RPTR-701Ns on one hand significantly reduced phagocytosis by RAW 264.7 cells as compared to PTR-701Ns, showing an immune escape effect. On the other hand, RPTR-701Ns had an advanced exotoxins neutralization ability, which helped reduce the damage of MRSA exotoxins to RBCs by 17.13%. Furthermore, excellent in vivo bacteria elimination and promoted wound healing were observed of RPTR-701Ns with a MRSA-infected mice model without causing toxicity. In summary, the novel delivery system provides a synergistic antibacterial treatment of both sustained release and bacterial toxins absorption, facilitating the incorporation of TR-701 into modern nanotechnology.

scholarly journals Active site remodelling accompanies thioester bond formation in the SUMO E1

Nature ◽  
2010 ◽  
Vol 463 (7283) ◽  
pp. 906-912 ◽  
Author(s):  
Shaun K. Olsen ◽  
Allan D. Capili ◽  
Xuequan Lu ◽  
Derek S. Tan ◽  
Christopher D. Lima
Keyword(s):  
Active Site ◽  
Bond Formation ◽  
Thioester Bond

Imidazolium-supported benzotriazole: an efficient and recoverable activating reagent for amide, ester and thioester bond formation in water

RSC Advances ◽  
2015 ◽  
Vol 5 (100) ◽  
pp. 82199-82207 ◽  
Author(s):  
S. M. Abdul Shakoor ◽  
Sunita Choudhary ◽  
Kiran Bajaj ◽  
Manoj Kumar Muthyala ◽  
Anil Kumar ◽  
...  
Keyword(s):  
Bond Formation ◽  
Carboxyl Group ◽  
Thioester Bond

An efficient and recyclable imidazolium-supported benzotriazole reagent (Im-CH2-BtH) as a novel synthetic auxiliary has been synthesized and explored for its carboxyl group activating capability for the synthesis of amides, esters and thioesters in water.

scholarly journals Dual encapsulation of hydrophobic and hydrophilic drugs in PLGA nanoparticles by a single-step method: drug delivery and cytotoxicity assays

RSC Advances ◽  
2016 ◽  
Vol 6 (112) ◽  
pp. 111060-111069 ◽  
Author(s):  
Laura Español ◽  
Ane Larrea ◽  
Vanesa Andreu ◽  
Gracia Mendoza ◽  
Manuel Arruebo ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Plga Nanoparticles ◽  
Single Step ◽  
Step Method ◽  
Drug Encapsulation ◽  
Hydrophilic Drugs ◽  
Biodegradable Nanoparticles ◽  
Cytotoxicity Assays ◽  
Dual Drug

Dual drug encapsulation in biodegradable nanoparticles is always challenging and often requires strenuous optimization of the synthesis–encapsulation processes.

scholarly journals Current therapeutic applications and pharmacokinetic modulations of ivermectin

2019 ◽  
Vol 12 (8) ◽  
pp. 1204-1211 ◽  
Author(s):  
Khan Sharun ◽  
T. S. Shyamkumar ◽  
V. A. Aneesha ◽  
Kuldeep Dhama ◽  
Abhijit Motiram Pawde ◽  
...  
Keyword(s):  
Sustained Release ◽  
Plasma Concentrations ◽  
Oral Route ◽  
Research Trend ◽  
Therapeutic Drug ◽  
Parasitic Diseases ◽  
Therapeutic Applications ◽  
Drug Concentrations ◽  
Wonder Drug ◽  
Long Acting

Ivermectin is considered to be a wonder drug due to its broad-spectrum antiparasitic activity against both ectoparasites and endoparasites (under class of endectocide) and has multiple applications in both veterinary and human medicine. In particular, ivermectin is commonly used in the treatment of different kinds of infections and infestations. By altering the vehicles used in the formulations, the pharmacokinetic properties of different ivermectin preparations can be altered. Since its development, various vehicles have been evaluated to assess the efficacy, safety, and therapeutic systemic concentrations of ivermectin in different species. A subcutaneous route of administration is preferred over a topical or an oral route for ivermectin due to superior bioavailability. Different formulations of ivermectin have been developed over the years, such as stabilized aqueous formulations, osmotic pumps, controlled release capsules, silicone carriers, zein microspheres, biodegradable microparticulate drug delivery systems, lipid nanocapsules, solid lipid nanoparticles, sustained-release ivermectin varnish, sustained-release ivermectin-loaded solid dispersion suspension, and biodegradable subcutaneous implants. However, several reports of ivermectin resistance have been identified in different parts of the world over the past few years. Continuous use of suboptimal formulations or sub-therapeutic plasma concentrations may predispose an individual to resistance toward ivermectin. The current research trend is focused toward the need for developing ivermectin formulations that are stable, effective, and safe and that reduce the number of doses required for complete clinical cure in different parasitic diseases. Therefore, single-dose long-acting preparations of ivermectin that provide effective therapeutic drug concentrations need to be developed and commercialized, which may revolutionize drug therapy and prophylaxis against various parasitic diseases in the near future. The present review highlights the current advances in pharmacokinetic modulation of ivermectin formulations and their potent therapeutic applications, issues related to emergence of ivermectin resistance, and future trends of ivermectin usage. Keywords: ivermectin, ivermectin resistance, pharmacokinetic modulation, therapeutic applications.

scholarly journals Evaluating the Mucoprotective Effects of Glycyrrhizic Acid Loaded Polymeric Nanoparticles Against 5-Fluorouracil Induced Intestinal Mucositis in Murine Model via Suppression of Inflammatory Mediators and Oxidative Stress

2021 ◽  
Author(s):  
Mahira Zeeshan ◽  
Ayesha Atiq ◽  
Qurat Ul Ain ◽  
Jawad Ali ◽  
Salman Khan ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Inflammatory Mediators ◽  
Glycyrrhizic Acid ◽  
Plga Nanoparticles ◽  
Therapeutic Effects ◽  
Therapeutic Action ◽  
Polymeric Nanocarriers ◽  
Intestinal Mucositis ◽  
Anti Inflammatory

Abstract Objectives: 5-Flourouracil (5-FU), a chemotherapeutic drug, is linked with severe deteriorating effects on intestine leading to mucositis. Further, Glycyrrhizic acid is a renown herbal medicine with combined mucoprotective, antioxidant and anti-inflammatory actions, however associated with pharmacokinetics limitations. Owing to its remarkable therapeutic action in inflammatory bowel disease inside the polymeric nanocarriers, we have tried to explore its activity against 5-FU led intestinal mucositis. Polymeric nanocarriers proved to be efficient drug delivery vehicles for long-term remedy against inflammatory diseases, however, yet not explored for 5-FU induced mucositis. Therefore, the study aimed to produce Glycyrrhizic acid loaded poly lactic-co-glycolic acid (GA-PLGA) nanoparticles to evaluate its protective and therapeutic effects on intestinal mucosa against 5-FU mediated mucositis. Methods: For the said purpose, GA-PLGA nanoparticles were prepared using modified double emulsion method, physicochemically characterized and tested for invitro drug release. Thereafter, mucositis was induced by 5-FU (50 mg/kg; IP) administration to the mice for the first three days (day 0, 1, 2) and orally treated with GA-PLGA nanoparticles till seventh day (day 0-6). Results: GA-PLGA nanoparticles significantly reduced mucositis severity as manifested through recovered body weight, diarrhea score, distress, and anorexia. Further, 5-FU induced intestinal histopathological damage, altered villi-crypt length, low goblet cell count, elevated pro-inflammatory mediators and suppressed antioxidant enzymes were reversed by GA-PLGA nanoparticles’ sustained release therapeutic action. Conclusion: Morphological, behavioral, histological, and biochemical results suggested that GA-PLGA nanoparticles found to be efficient, biocompatible, targeted, sustained release drug delivery nano-vehicle for enhanced mucoprotective, anti-inflammatory and antioxidant effects in ameliorating 5-FU intestine mucositis.

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