scholarly journals Design of targeted dosage form of ofloxacin+

2006 ◽  
Vol 71 (12) ◽  
pp. 1269-1273 ◽  
Author(s):  
Yar Shahar ◽  
Ahamed Siddiqui ◽  
Ashraf Ali ◽  
E. Manogran
Keyword(s):  
Drug Design ◽  
Specific Activity ◽  
In Vitro Release ◽  
Polymer Backbone ◽  
Specific Chemical ◽  
Site Specific ◽  
Development Of Resistance ◽  
Quinolone Antibiotics ◽  
New Strategy

The targeted pro-drug is a classical pro-drug design often representing a non-specific chemical approach to mask undesirable drug properties, such as limited bioavailability, lack of site specificity, and chemical instability. On the other hand, targeted pro-drug design represents a new strategy for directed and efficient drug delivery. Quinolone antibiotics exert their pharmacological effect by inhibiting the cell wall synthesis of the pathogen. However, development of resistance exists, which instigates for a new higher congener to remain in clinical practice. To overcome this phenomenon and also to produce site-specific activity of the cell walls of the pathogen, ofloxacin is conjugated with a hydroxypropyl methacrylamide polymer backbone moiety. The results of in vitro release studies indicate the possibilities for the development of a new drug for site-specific therapy with an improved t 1/2 of the drug. This novel pro-drugmay have opened a new vista in antibiotic chemotherapy. .

scholarly journals Clotrimazole-Loaded Mediterranean Essential Oils NLC: A Synergic Treatment of Candida Skin Infections

Pharmaceutics ◽  
2019 ◽  
Vol 11 (5) ◽  
pp. 231 ◽  
Author(s):  
Claudia Carbone ◽  
Maria do Céu Teixeira ◽  
Maria do Céu Sousa ◽  
Carlos Martins-Gomes ◽  
Amelia M. Silva ◽  
...  
Keyword(s):  
Essential Oils ◽  
Cell Line ◽  
Synergistic Effects ◽  
In Vitro Release ◽  
Skin Infections ◽  
Candida Spp ◽  
Drug Effectiveness ◽  
Development Of Resistance ◽  
Calorimetric Studies

The increasing development of resistance of Candida species to traditional drugs represents a great challenge to the medical field for the treatment of skin infections. Essential oils were recently proposed to increase drug effectiveness. Herein, we developed and optimized (23 full factorial design) Mediterranean essential oil (Rosmarinus officinalis, Lavandula x intermedia “Sumian”, Origanum vulgare subsp. hirtum) lipid nanoparticles for clotrimazole delivery, exploring the potential synergistic effects against Candida spp. Small sized nanoparticles (<100 nm) with a very broad size distribution (PDI < 0.15) and long-term stability were successfully prepared. Results of the in vitro biosafety on HaCaT (normal cell line) and A431 (tumoral cell line), allowed us to select Lavandula and Rosmarinus as anti-proliferative agents with the potential to be used as co-adjuvants in the treatment of non-tumoral proliferative dermal diseases. Results of calorimetric studies on biomembrane models, confirmed the potential antimicrobial activity of the selected oils due to their interaction with membrane permeabilization. Nanoparticles provided a prolonged in vitro release of clotrimazole. In vitro studies against Candida albicans, Candida krusei and Candida parapsilosis, showed an increase of the antifungal activity of clotrimazole-loaded nanoparticles prepared with Lavandula or Rosmarinus, thus confirming nanostructured lipid carriers (NLC) containing Mediterranean essential oils represent a promising strategy to improve drug effectiveness against topical candidiasis.

Sugar-based poly (anhydride-ester) containing natural antioxidants and antimicrobials: Synthesis and formulation into polymer blends

2016 ◽  
Vol 32 (2) ◽  
pp. 196-208 ◽  
Author(s):  
Nicholas D Stebbins ◽  
Michelle M Moy ◽  
Jonathan J Faig ◽  
Kathryn E Uhrich
Keyword(s):  
High Temperature ◽  
In Vitro Release ◽  
Radical Scavenging ◽  
Natural Antioxidants ◽  
Antimicrobial Activities ◽  
Polymer Backbone ◽  
Naturally Occurring ◽  
Release Studies ◽  
Vitro Release

Thymol, a naturally occurring antioxidant and antimicrobial, is commonly researched for active packaging applications to deter food spoilage and bacterial growth. However, the high temperature necessary for processing often volatilizes the thymol, reducing its utility. To overcome this processing limitation, sugar-based poly(anhydride-esters) comprising thymol and compounds generally regarded as safe (succinic and tartaric acid) were successful prepared via mild solution polymerization methods. In vitro release studies demonstrated a sustained thymol release over 3 weeks at therapeutically relevant concentrations. Furthermore, the released thymol displayed antioxidant and antimicrobial activities as indicated by a 2,2-diphenyl-1-picrylhydrazyl radical scavenging and Kirby–Bauer disk diffusion assays, respectively. High-temperature melt blending with low-density polyethylene revealed that the chemical incorporation of thymol into a polymer backbone overcame volatility issues and maintained relevant bioactivity.

scholarly journals Candida albicansVMA3Is Necessary for V-ATPase Assembly and Function and Contributes to Secretion and Filamentation

2013 ◽  
Vol 12 (10) ◽  
pp. 1369-1382 ◽  
Author(s):  
Hallie S. Rane ◽  
Stella M. Bernardo ◽  
Summer M. Raines ◽  
Jessica L. Binder ◽  
Karlett J. Parra ◽  
...  
Keyword(s):  
Atpase Activity ◽  
Cellular Response ◽  
Specific Activity ◽  
Calcium Sensitivity ◽  
Vacuolar Membrane ◽  
Cold Sensitivity ◽  
Specific Chemical ◽  
Content Type ◽  
Concanamycin A

ABSTRACTThe vacuolar membrane ATPase (V-ATPase) is a protein complex that utilizes ATP hydrolysis to drive protons from the cytosol into the vacuolar lumen, acidifying the vacuole and modulating several key cellular response systems inSaccharomyces cerevisiae. To study the contribution of V-ATPase to the biology and virulence attributes of the opportunistic fungal pathogenCandida albicans, we created a conditional mutant in whichVMA3was placed under the control of a tetracycline-regulated promoter (tetR-VMA3strain). Repression ofVMA3in the tetR-VMA3strain prevents V-ATPase assembly at the vacuolar membrane and reduces concanamycin A-sensitive ATPase-specific activity and proton transport by more than 90%. Loss ofC. albicansV-ATPase activity alkalinizes the vacuolar lumen and has pleiotropic effects, including pH-dependent growth, calcium sensitivity, and cold sensitivity. The tetR-VMA3strain also displays abnormal vacuolar morphology, indicative of defective vacuolar membrane fission. The tetR-VMA3strain has impaired aspartyl protease and lipase secretion, as well as attenuated virulence in anin vitromacrophage killing model. Repression ofVMA3suppresses filamentation, and V-ATPase-dependent filamentation defects are not rescued by overexpression ofRIM8,MDS3,EFG1,CST20, orUME6, which encode positive regulators of filamentation. Specific chemical inhibition of Vma3p function also results in defective filamentation. These findings suggest either that V-ATPase functions downstream of these transcriptional regulators or that V-ATPase function during filamentation involves independent mechanisms and alternative signaling pathways. Taken together, these data indicate that V-ATPase activity is a fundamental requirement for several key virulence-associated traits inC. albicans.

Multi-kinetics and site-specific release of gabapentin and flurbiprofen from oral fixed-dose combination: in vitro release and in vivo food effect

2017 ◽  
Vol 262 ◽  
pp. 296-304 ◽  
Author(s):  
Fabio Sonvico ◽  
Chiara Conti ◽  
Gaia Colombo ◽  
Francesca Buttini ◽  
Paolo Colombo ◽  
...  
Keyword(s):  
Food Effect ◽  
In Vitro Release ◽  
Fixed Dose Combination ◽  
Fixed Dose ◽  
Site Specific ◽  
Dose Combination ◽  
Vitro Release

scholarly journals Utilization of LC-MS/MS Analyses to Identify Site-Specific Chemical Protein Adducts In Vitro

2010 ◽  
pp. 317-326 ◽  
Author(s):  
Ashley A. Fisher ◽  
Matthew T. Labenski ◽  
Terrence J. Monks ◽  
Serrine S. Lau
Keyword(s):  
Protein Adducts ◽  
Specific Chemical ◽  
Site Specific

scholarly journals Drug design of anti-covid19 agents

2020 ◽  
Author(s):  
Pardis Tabaee Damavandi
Keyword(s):  
Drug Design ◽  
Extended Release ◽  
Lung Surfactant ◽  
Antiviral Agents ◽  
Lung Surfactants ◽  
Specific Design ◽  
Site Specific ◽  
Pediatric Use ◽  
The Individual

The first step to drug development that precedes formulation is drug design. In this commentary the specific design of antiviral agents for Covid19 and future viruses, which can be achieved with different strategies, is highlighted. An extended release type of formulation would be ideal for site-specific antivirals however early in vitro or toxicology screening is very important. A lot of preparations are already available to be exploited. Conversely, some are available for pediatric use, i.e lung surfactants, which understandably the supply of is aimed at premature children. New lung surfactant design for adults could however be also incentivised which may help re-establishing autonomous respiration (autonomically mediated) post-covid19 infection of the individual. The surfactants could also help counteract dyspnea which is sometimes a known side effect of antiviral agents.

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