FSE–Ag complex NS: preparation and evaluation of antibacterial activity

Kalhapure, Rahul S.; Bolla, Pradeep Kumar; Domı́nguez, Delfina C.; Dahal, Amit; Boddu, Sai H. S.; Renukuntla, Jwala

doi:10.1049/iet-nbt.2017.0284

Cited by 6 publications

(5 citation statements)

References 31 publications

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“…Crystalline nature of the compounds effects important properties such as stability, solubility, and bioavailability. Amorphous forms of drug molecules are characterized with higher solubilities and increased bioavailability [33,34]. XRD diffractograms for clotrimazole, cholesterol, sodium oleate and clotrimazole loaded ufosomes are provided in Figure 4.…”

Section: Resultsmentioning

confidence: 99%

Clotrimazole Loaded Ufosomes for Topical Delivery: Formulation Development and In-Vitro Studies

et al. 2019

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Global incidence of superficial fungal infections caused by dermatophytes is high and affects around 40 million people. It is the fourth most common cause of infection. Clotrimazole, a broad spectrum imidazole antifungal agent is widely used to treat fungal infections. Conventional topical formulations of clotrimazole are intended to treat infections by effective penetration of drugs into the stratum corneum. However, drawbacks such as poor dermal bioavailability, poor penetration, and variable drug levels limit the efficiency. The present study aims to load clotrimazole into ufosomes and evaluate its topical bioavailability. Clotrimazole loaded ufosomes were prepared using cholesterol and sodium oleate by thin film hydration technique and evaluated for size, polydispersity index, and entrapment efficiency to obtain optimized formulation. Optimized formulation was characterized using scanning electron microscopy (SEM), X-ray diffraction (XRD), and differential scanning calorimetry (DSC). Skin diffusion studies and tape-stripping were performed using human skin to determine the amount of clotrimazole accumulated in different layers of the skin. Results showed that the optimized formulation had vesicle size <250 nm with ~84% entrapment efficiency. XRD and DSC confirmed the entrapment of clotrimazole into ufosomes. No permeation was observed through the skin up to 24 h following the permeation studies. Tape-stripping revealed that ufosomes led to accumulation of more clotrimazole in the skin compared to marketed formulation (Perrigo). Overall, results revealed the capability of ufosomes in improving the skin bioavailability of clotrimazole.

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Section: Resultsmentioning

confidence: 99%

Clotrimazole Loaded Ufosomes for Topical Delivery: Formulation Development and In-Vitro Studies

et al. 2019

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“…Subsequently, a comparative analysis was conducted between the IR spectra of the physical amalgamation and those of the individual pure medication and polymers, aiming to discern any potential incompatibilities or interactions among the components. [20]…”

Section: Fourier Transform Infrared Spectroscopy (Ftir)mentioning

confidence: 99%

"Optimizing Pharmaceutical Formulations: Advancements in Nanosuspension Pre-Formulation to Enhance Solubility and Bioavailability of Active Agents"

Bhosale,

Singh

2023

ijmst

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This study aimed to enhance the bioavailability of a poorly water soluble drug by developing a nanosuspension through an innovative formulation method. The nanosuspension was produced with meticulous attention to the materials reliability and excellent quality. Nepafenac was characterised in the pre-formulation study by establishing its melting point, solubility in different solvents, organoleptic properties, and creating a calibration curve. We utilised UV spectroscopy to determine the maximum wavelength (?max) of Nepafenac and construct a standard calibration curve in ethanol. To ensure the compatibility of the medicine with the polymers (Pluronic F127 and HPMC E 5), Fourier Transform Infrared Spectroscopy (FTIR) was utilised for drug interaction analysis. The nanosuspension was produced using the solvent diffusion approach. The effect of different concentrations of Poloxamer 407 and HPMC E 5 on the formulation's effectiveness was investigated experimentally using a 32 complete factorial design. We used Response Surface Methodology (RSM) and statistical analysis to enhance the formulation concerning in vitro release, particle size, and viscosity. The pre-formulation characteristics of Nepafenac met the standards outlined in the Pharmacopoeial regulations. The maximum absorption wavelength (?max) of Nepafenac was confirmed by UV spectroscopy, and a reliable calibration curve was created. The FTIR analysis showed no chemical interaction between the medicine and polymers. RSM and experimental design indicated that Poloxamer 407 and HPMC E 5 had a substantial impact on the performance of the nanosuspension. Analysis of variance (ANOVA) confirmed the model and parameters that influence controlled drug release percentage, particle size, and viscosity. Optimal conditions for enhancing drug delivery and reducing particle size were determined by the analysis of contour and response surface plots. The optimal parameter values, as indicated in the desirability plots, closely matched the anticipated values. The experimentation confirmed the viability and effectiveness of the nanosuspension formulation generated based on the RSM findings.

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“…%EE was determined by using ultrafiltration method using Amicon ® Ultra-4 centrifugal filter tubes (Millipore Corp., USA) of 10 kDa pore size [34][35][36]. Polymersomes (2 mL) were placed in ultracentrifugal filter tube and centrifuged at 10,000 rpm for 20 min at 20 • C to separate unentrapped furosemide.…”

Section: Determination Of Encapsulation Efficiency (%Ee)mentioning

confidence: 99%

Evaluation of Oleic Acid and Polyethylene Glycol Monomethyl Ether Conjugate (PEGylated Oleic Acid) as a Solubility Enhancer of Furosemide

et al. 2019

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Poor aqueous solubility limits the therapeutic efficacy of many marketed and investigational drugs. Synthesis of new drugs with improved solubility is challenging due to time constraint and expenses involved. Therefore, finding the solubility enhancers for existing drugs is an attractive and profitable strategy. In this study, PEGylated oleic acid (OA-mPEG5000), a conjugate of oleic acid and mPEG5000 was synthesized and evaluated as a solubilizer for furosemide. OA-mPEG5000 was evaluated as a nanocarrier for furosemide by formulating polymersomes. Solubility of furosemide in milli-Q water and aqueous OA-mPEG5000 solution was determined using shake flask method. At 37 °C, the solubility of furosemide in OA-mPEG5000 (1% w/w) and milli-Q water was 3404.7 ± 254.6 µg/mL and 1020.2 ± 40.9 µg/mL, respectively. Results showed there was a 3.34-fold increase in solubility of furosemide in OA-mPEG5000 compared to water at 37 °C. At 25 °C, there was a 3.31-fold increase in solubilization of furosemide in OA-mPEG5000 (1% w/w) (90.0 ± 1.45 µg/mL) compared to milli-Q water (27.2 ± 1.43 µg/mL). Size, polydispersity index and zeta potential of polymersomes ranged from 85–145.5 nm, 0.187–0.511 and −4.0–12.77 mV, respectively. In-vitro release study revealed a burst release (71%) within 1 h. Significant enhancement in solubility and formation of polymersomes suggested that OA-mPEG5000 could be a good solubilizer and nanocarrier for furosemide.

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FSE–Ag complex NS: preparation and evaluation of antibacterial activity

Cited by 6 publications

References 31 publications

Clotrimazole Loaded Ufosomes for Topical Delivery: Formulation Development and In-Vitro Studies

Clotrimazole Loaded Ufosomes for Topical Delivery: Formulation Development and In-Vitro Studies

"Optimizing Pharmaceutical Formulations: Advancements in Nanosuspension Pre-Formulation to Enhance Solubility and Bioavailability of Active Agents"

Evaluation of Oleic Acid and Polyethylene Glycol Monomethyl Ether Conjugate (PEGylated Oleic Acid) as a Solubility Enhancer of Furosemide

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