In this work, a new polymeric prodrug was successfully synthesized by Fischer-esterification between chitosan as biodegradable polymer and levofloxacin as drug material. Levofloxacin was linked directly to the chitosan through a degradable ester bond at (chitosan: levofloxacin) ratios of (1:1), (1:2), and (2:1). The resulting product was characterized by Fourier transform infrared spectroscopy, ultraviolet spectroscopy, thermogravimetric analysis, and differential scanning calorimetry to confirm its structure. Furthermore, the physical properties of the product were determined. The polymer-drug conjugate was evaluated for its drug content and in vitro drug release at pH 1.2 at a condition similar to physiological conditions. Profile of the in vitro drug release showed that levofloxacin was released in a sustained manner from pro(1:2). A high swelling index for pro(1:2) confirmed this finding. Therefore, the ester bond hydrolyzed in acidic media to release the drug. Antibacterial assay was conducted for synthesized prodrug against Pseudomonas aeruginosa, Escherichia coli, and Staphylococcus aureus species. The polymeric prodrug could be used successfully as a controlled drug delivery system.
Antacids have been widely used in the treatment of various gastric and duodenal disorders such as heartburn, reflux esophagitis, gastritis, irritable stomach, gastric and duodenal ulcers. A pH-responsive of bi-polymer of sodium alginate and pectin have been studied as raft-forming polymers using sodium bicarbonate and calcium carbonate as gas-generating and calcium ion sources. The aim of study was to formulate and evaluate mono and bilayer tablets of floating and sustained release antacid delivery systems using sodium carboxy methyl cellulose as a gel forming substance, calcium and magnesium carbonate as sources of acid neutralizing and carbon dioxide gas generators agents upon contact with acidic solution. The effect of the formulation contents on the buoyancy has been investigated. In addition to, the antacid activities of intact and pulverized tablets have been studied. The result obtained showed that the buoyance is remarkably affected by the percentages of sodium carboxy methyl cellulose and carbonates salts. All formulas of mono and bilayer tablets revealed sustained action of acid neutralization and raft formation. Besides, bilayer tablets showed a significant and higher level of acid neutralizing capacity than monolayer tablets. Moreover, the pulverized of bilayer tablets exhibited significant and higher acid neutralizing capacity at raft than that at bulk of artificial gastric juice medium. Keywords: Raft forming agent, Antacid, floating drug delivery, Acid neutralizing capacity, Sodium carboxy methyl cellulose.
Multidrug resistance has resulted in hurtful infections on treatment with common antimicrobials and is associated with health threatening problems. Antibiotic abuse in health care systems contributes to global resistance. β-lactams are the predominantly used antibiotics, and the most often used is cefotaxime, therefore facing a resistance problem. Potent cephalosporin derivatives, β-lactamase inhibitors, prodrugs, and drug nano-carriers are approaches to cutback bacterial resistance. An example of a nanocarrier applied in field of antibacterial activity enhancement is niosomes. Niosomes are self-assembled vesicles made from non-ionic surfactants with cholesterol also additives included or omitted that can provide good features such as antibiotic shielding, cleavage proofing, controlled release, and specific targeting. Cefotaxime niosomes preparation done by Thin-Film Hydration method using Tween 40, span 60, stearylamine, and cholesterol. The dried film was moisturised with buffered solution of cefotaxime at 45-55°C then the final nanosized niosomal cefotaxime was generated through a probe sonication. A 27 formulas were prepared and identified by dynamic light scattering so that polydispersity index and the vesicular size are measured. The selected formula of cefotaxime niosomes (CN6) has as showed the lowermost values and a prominent vesicular structure of 106 nm diameter on Transmission electron microscope and compatibility on Fourier Transform Infrared System analysis. CN6 remained unchanged in diameter and Poly-dispersity index after 100 days of storage at 2 to-80 C and also onsubsequent freeze drying and reconstitution. Entrapment efficiency was quantified by the ultracentrifugation method and was discovered to be 93 %. Antibiotic delivery by cefotaxime-eluting niosomes has been shown to be successful with antibacterial potentiation of 160, 8, 640 and 40 times better than aqueous solution against Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa respectively which is obviously a considerable drop in the minimum inhibitory concentrations of the selected formula versus the aqueous cefotaxime solution and this was evaluated using Agar well diffusion technique.
Anastrozole (ANZ) is a potent non-steroidal aromatase II inhibitor (AI) used to decrease or delay the progression of breast tumor growth in some women. Since ANZ could be delivered transdermally due to its physicochemical characteristics as (log p of 3.5, aqueous solubility of 0.5 mg /mL, low dosage and half-life of 46.8 hr.) so, it could be used as a modelling drug evaluation of ethosomes, the current study aimed to formulate ANZ loaded ethosomes and evaluate the formulated ethosomes for particle size and PDI, entrapment efficiency and in vitro release profile. Film hydration method was used to prepare ANZ-loaded ethosoms. using different ratios of phospholipid (Soy phosphatidyl choline) and ethanol at variables probe sonication energy and time ratios. polydispersity index and particle size were used to evaluate the prepared ANZ-loaded ethosoms. The optimized formula of ethosomes which contain (1% Soy phosphatidyl choline,20% ethanol subjected to 300watt sonication energy with 1/3 sonication on /off ratio) was studied for in vitro drug release. It had 127.75±0.36 nm particle diameter and 74.7136 ± 3.457 % entrapment efficiency, the release kinetics obey Korsmeyer-Peppas and non-Fickian release as R2=0.9779 and n=0.737. The ratios of Soy phosphatidyl choline, ethanol, sonication energy and duration had a significant impact on the particle size of ethosomes at (p0.05). The preformulating analysis of Powder X-ray diffraction (P-XRD) indicate amorphous ethosomes. Fourier transform infrared (FTIR) showed the inertness among components.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
hi@scite.ai
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.