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1.
Molecules ; 26(16)2021 Aug 05.
Artigo em Inglês | MEDLINE | ID: mdl-34443336

RESUMO

We develop a suitable delivery system for niaouli essential oil (NEO) using a nanoemulsification method for acne vulgaris. Prepared nanoemulsions (NEs) were characterized for droplet dimension, rheology, surface charge, and stability. The ability of NEO formulations against Propionibacterium acnes and Staphylococcus epidermidis was investigated and all formulations showed antiacne potential in vitro. Ex vivo permeation studies indicated significant improvement in drug permeations and steady state flux of all NEO-NEs compared to the neat NEO (p < 0.05). On the basis of the studied pharmaceutical parameters, enhanced ex vivo skin permeation, and marked effect on acne pathogens, formulation NEO-NE4 was found to be the best (oil (NEO; 10% v/v); Kolliphor EL (9.25% v/v), Carbitol (27.75% v/v), and water (53% v/v)). Concisely, the in vitro and ex vivo results revealed that nanoemulsification improved the delivery as well as bioactivities of NEO significantly.


Assuntos
Portadores de Fármacos/química , Melaleuca/química , Nanoestruturas/química , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Emulsões , Óleos Voláteis/metabolismo , Permeabilidade , Pele/metabolismo , Staphylococcus epidermidis/efeitos dos fármacos
2.
Phytochem Anal ; 2021 Jul 05.
Artigo em Inglês | MEDLINE | ID: mdl-34227167

RESUMO

INTRODUCTION: Thymoquinone (TQ) is a naturally derived bioactive compound with several therapeutic effects. OBJECTIVE: The highly sensitive, rapid and green normal-phase (NP)/reversed-phase (RP) high-performance thin-layer chromatography (HPTLC) densitometry technique was developed for the determination of TQ in various plant extracts of different geographical regions, commercial capsules, creams and essential oils. METHODOLOGY: The NP densitometry estimation of TQ was performed using a cyclohexane-ethyl acetate (90:10, v/v) green solvent system, while, the RP-densitometry estimation of TQ was performed using an ethanol-water (80:20, v/v) green solvent system. The estimation of TQ was conducted at 259 nm. RESULTS: The NP and RP densitometry techniques were observed linear in the range of 25-1000 and 50-600 ng/band, respectively. All validation parameters such as accuracy, precision, robustness and sensitivity of NP/RP densitometry were observed within the limit of regulatory requirements and hence found to be suitable for the determination of TQ. The TQ contents were found to be highest in the Saudi Arabian extract followed by the Syrian extract, Indian extract, commercial capsules, commercial creams, Jordanian extract, Egyptian extract, Palestinian extract and commercial essential oils using NP densitometry. The TQ contents were found in same order using RP densitometry, but they were much lower than those recorded using NP densitometry. The Analytical GREEnness (AGREE) scores of NP and RP densitometry were found to be 0.82 and 0.84, respectively, suggesting an excellent greenness profile. CONCLUSIONS: Based on these results, NP/RP densitometry was found to be suitable for the pharmaceutical assay of TQ.

3.
Molecules ; 26(11)2021 May 21.
Artigo em Inglês | MEDLINE | ID: mdl-34064283

RESUMO

This research deals with the determination of solubility, Hansen solubility parameters, dissolution properties, enthalpy-entropy compensation, and computational modeling of a naturally-derived bioactive compound trans-resveratrol (TRV) in water, methanol, ethanol, n-propanol, n-butanol, propylene glycol (PG), and various PG + water mixtures. The solubility of TRV in six different mono-solvents and various PG + water mixtures was determined at 298.2-318.2 K and 0.1 MPa. The measured experimental solubility values of TRV were regressed using six different computational/theoretical models, including van't Hoff, Apelblat, Buchowski-Ksiazczak λh, Yalkowsly-Roseman, Jouyban-Acree, and van't Hoff-Jouyban-Acree models, with average uncertainties of less than 3.0%. The maxima of TRV solubility in mole fraction was obtained in neat PG (2.62 × 10-2) at 318.2 K. However, the minima of TRV solubility in the mole fraction was recorded in neat water (3.12 × 10-6) at 298.2 K. Thermodynamic calculation of TRV dissolution properties suggested an endothermic and entropy-driven dissolution of TRV in all studied mono-solvents and various PG + water mixtures. Solvation behavior evaluation indicated an enthalpy-driven mechanism as the main mechanism for TRV solvation. Based on these data and observations, PG has been chosen as the best mono-solvent for TRV solubilization.


Assuntos
Propilenoglicol/química , Resveratrol/química , Solventes/química , Água/química , Modelos Químicos , Solubilidade , Termodinâmica , Incerteza
4.
Molecules ; 26(11)2021 May 26.
Artigo em Inglês | MEDLINE | ID: mdl-34073527

RESUMO

This article studies the solubility, Hansen solubility parameters (HSPs), and thermodynamic behavior of a naturally-derived bioactive thymoquinone (TQ) in different binary combinations of isopropanol (IPA) and water (H2O). The mole fraction solubilities (x3) of TQ in various (IPA + H2O) compositions are measured at 298.2-318.2 K and 0.1 MPa. The HSPs of TQ, neat IPA, neat H2O, and binary (IPA + H2O) compositions free of TQ are also determined. The x3 data of TQ are regressed by van't Hoff, Apelblat, Yalkowsky-Roseman, Buchowski-Ksiazczak λh, Jouyban-Acree, and Jouyban-Acree-van't Hoff models. The maximum and minimum x3 values of TQ are recorded in neat IPA (7.63 × 10-2 at 318.2 K) and neat H2O (8.25 × 10-5 at 298.2 K), respectively. The solubility of TQ is recorded as increasing with the rise in temperature and IPA mass fraction in all (IPA + H2O) mixtures, including pure IPA and pure H2O. The HSP of TQ is similar to that of pure IPA, suggesting the great potential of IPA in TQ solubilization. The maximum molecular solute-solvent interactions are found in TQ-IPA compared to TQ-H2O. A thermodynamic study indicates an endothermic and entropy-driven dissolution of TQ in all (IPA + H2O) mixtures, including pure IPA and pure H2O.


Assuntos
2-Propanol/química , Benzoquinonas/química , Química Farmacêutica/métodos , Água/química , Técnicas de Química Analítica , Desenho de Fármacos , Análise de Regressão , Reprodutibilidade dos Testes , Solubilidade , Solventes , Temperatura , Termodinâmica
5.
PLoS One ; 16(4): e0249485, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33831070

RESUMO

The aim of this work was to solubilize simvastatin (SIM) using different micellar solutions of various non-ionic surfactants such as Tween-80 (T80), Tween-20 (T20), Myrj-52 (M52), Myrj-59 (M59), Brij-35 (B35) and Brij-58 (B58). The solubility of SIM in water (H2O) and different micellar concentrations of T80, T20, M52, M59, B35 and B58 was determined at temperatures T = 300.2 K to 320.2 K under atmospheric pressure p = 0.1 MPa using saturation shake flask method. The experimental solubility data of SIM was regressed using van't Hoff and Apelblat models. The solubility of SIM (mole fraction) was recorded highest in M59 (1.54 x 10-2) followed by M52 (6.56 x 10-3), B58 (5.52 x 10-3), B35 (3.97 x 10-3), T80 (1.68 x 10-3), T20 (1.16 x 10-3) [the concentration of surfactants was 20 mM in H2O in all cases] and H2O (1.94 x 10-6) at T = 320.2 K. The same results were also recorded at each temperature and each micellar concentration of T80, T20, M52, M59, B35 and B58. "Apparent thermodynamic analysis" showed endothermic and entropy-driven dissolution/solubilization of SIM in H2O and various micellar solutions of T80, T20, M52, M59, B35 and B58.


Assuntos
Micelas , Modelos Moleculares , Sinvastatina/química , Tensoativos/química , Conformação Molecular , Polietilenoglicóis/química , Solubilidade , Solventes/química , Termodinâmica , Água/química
6.
Drug Dev Ind Pharm ; 47(4): 654-662, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-33823120

RESUMO

The solubilization, Hansen solubility parameters (HSPs), and thermodynamic properties of delafloxacin (DLN) in various unique combination of Transcutol-HP® (THP) and 1-butyl-3-methyl imidazolium hexafluorophosphate ionic liquid (BMIM-PF6) mixtures were evaluated for the first time in this research. The 'mole fraction solubilities (x3)' of DLN in different (THP + BMIM-PF6) compositions were determined at 'T = 298.2-318.2 K' and 'p = 0.1 MPa'. The HSPs of DLN, neat THP, neat BMIM-PF6, and binary (THP + BMIM-PF6) compositions free of DLN were also determined. The x3 data of DLN was regressed using 'van't Hoff, Apelblat, Yalkowsky-Roseman, Jouyban-Acree and Jouyban-Acree-van't Hoff models' with overall error values of less than 3.0%. The highest and lowest x3 value of DLN was recorded in neat THP (5.48 × 10-3 at T = 318.2 K) and neat BMIM-PF6 (6.50 × 10-4 at T = 298.2 K), respectively. The solubility of DLN was found to be enhanced significantly with an arise in temperature in all (THP + BMIM-PF6) compositions including pure THP and pure BMIM-PF6. However, there was slight increase in DLN solubility with increase in THP mass fraction in all (THP + BMIM-PF6) mixtures. The HSP of pure THP and pure BMIM-PF6 were found very close to each other, suggesting the great potential of both solvents in DLN solubilization. The maximum solute-solvent interactions at molecular level were recorded in DLN-THP compared to DLN-BMIM-PF6. An 'apparent thermodynamic analysis' study indicated an 'endothermic and entropy-driven dissolution' of DLN in all (THP + BMIM-PF6) compositions including neat THP and BMIM-PF6.


Assuntos
Água , Etilenoglicóis , Fluoroquinolonas , Solubilidade , Termodinâmica
7.
Pharmaceutics ; 13(3)2021 Mar 10.
Artigo em Inglês | MEDLINE | ID: mdl-33802156

RESUMO

Recently, drug delivery using natural biological carriers has emerged as one of the most widely investigated topics of research. Erythrocytes, or red blood cells, can act as potential carriers for a wide variety of drugs, including anticancer, antibacterial, antiviral, and anti-inflammatory, along with various proteins, peptides, enzymes, and other macromolecules. The red blood cell-based nanocarrier systems, also called nanoerythrosomes, are nanovesicles poised with extraordinary features such as long blood circulation times, the ability to escape immune system, the ability to release the drug gradually, the protection of drugs from various endogenous factors, targeted and specified delivery of drugs, as well as possessing both therapeutic and diagnostic applications in various fields of biomedical sciences. Their journey over the last two decades is escalating with fast pace, ranging from in vivo to preclinical and clinical studies by encapsulating a number of drugs into these carriers. Being biomimetic nanoparticles, they have enhanced the stability profile of drugs and their excellent site-specific targeting ability makes them potential carrier systems in the diagnosis and therapy of wide variety of tumors including gliomas, lung cancers, breast cancers, colon cancers, gastric cancers, and other solid tumors. This review focuses on the most recent advancements in the field of nanoerythrosomes, as an excellent and promising nanoplatform for the novel drug delivery of various drugs particularly antineoplastic drugs along with their potential as a promising diagnostic tool for the identification of different tumors.

8.
Foods ; 10(3)2021 Mar 13.
Artigo em Inglês | MEDLINE | ID: mdl-33805719

RESUMO

This study aimed to perform a systematic review on gluten-free bread formulations using specific volumes as a quality indicator. In this systematic review, we identified 259 studies that met inclusion criteria. From these studies, 43 met the requirements of having gluten-free bread with a specific volume greater than or equal to 3.5 cm3/g. Other parameters such as the texture profile, color (crumb and crust), and sensory analysis examined in these studies were presented. The formulations that best compensated the lack of the gluten-network were based on the combination of rice flour, rice flour with low amylose content, maize flour, rice starch, corn starch, potato starch, starch with proteins and added with transglutaminase (TGase), and hydrocolloids like hydroxypropylmethylcellulose (HPMC). Of the 43 studies, three did not present risk of bias, and the only parameter evaluated in common in the studies was the specific volume. However, it is necessary to jointly analyze other parameters that contribute to the quality, such as texture profile, external and internal characteristics, acceptability, and useful life of the bread, especially since it is a product obtained through raw materials and unconventional ingredients.

9.
Molecules ; 26(7)2021 Apr 03.
Artigo em Inglês | MEDLINE | ID: mdl-33916710

RESUMO

A wide range of analytical techniques are reported for the determination of cinnamaldehyde (CCHO) and eugenol (EOH) in plant extracts and herbal formulations either alone or in combination. Nevertheless, sustainable/green analytical techniques for the estimation of CCHO and EOH either alone or in combination are scarce in the literature. Accordingly, the present research was carried out to establish a rapid, highly sensitive, and sustainable high-performance thin-layer chromatography (HPTLC) technique for the simultaneous estimation of CCHO and EOH in the traditional and ultrasound-assisted methanolic extracts of Cinnamomum zeylanicum,C. burmannii, and C. cassia and their essential oils. The simultaneous estimation of CCHO and EOH was performed through NP-18 silica gel 60 F254S HPTLC plates. The cyclohexane/ethyl acetate (90:10, v v-1) solvent system was optimized as the mobile phase for the simultaneous estimation of CCHO and EOH. The greenness score of the HPTLC technique was predicted using AGREE software. The entire analysis was carried out at a detection wavelength of 296 nm for CCHO and EOH. The sustainable HPTLC technique was observed as linear in the range 10-2000 ng band-1 for CCHO and EOH. The proposed technique was found to be highly sensitive, rapid, accurate, precise, and robust for the simultaneous estimation of CCHO and EOH. The content of CCHO in traditional methanolic extracts of C. zeylanicum,C. burmannii, and C. cassia was found to be 96.36, 118.49, and 114.18 mg g-1, respectively. However, the content of CCHO in ultrasound-assisted methanolic extracts of C. zeylanicum,C. burmannii, and C. cassia was found to be 111.57, 134.39, and 129.07 mg g-1, respectively. The content of CCHO in essential oils of C. zeylanicum,C. burmannii, and C. cassia was found to be 191.20, 214.24, and 202.09 mg g-1, respectively. The content of EOH in traditional methanolic extracts of C. zeylanicum,C. burmannii, and C. cassia was found to be 73.38, 165.41, and 109.10 mg g-1, respectively. However, the content of EOH in ultrasound-assisted methanolic extracts of C. zeylanicum,C. burmannii, and C. cassia was found to be 87.20, 218.09, and 121.85 mg g-1, respectively. The content of EOH in essential oils of C. zeylanicum,C. burmannii, and C. cassia was found to be 61.26, 79.21, and 69.02 mg g-1, respectively. The amounts of CCHO and EOH were found to be significantly higher in ultrasound-assisted extracts of all species compared to its traditional extraction and hence ultrasound extraction has been proposed as a superior technique for the extraction of CCHO and EOH. The AGREE analytical score of the present analytical technique was predicted as 0.75, suggesting excellent greenness profile of the proposed analytical technique. Based on all these observations and results, the proposed sustainable HPTLC technique can be successfully used for the simultaneous estimation of CCHO and EOH in different plant extracts and herbal products.


Assuntos
Acroleína/análogos & derivados , Cromatografia em Camada Delgada , Cinnamomum zeylanicum/química , Eugenol/análise , Química Verde , Óleos Voláteis/química , Extratos Vegetais/química , Ultrassom , Acroleína/análise , Análise dos Mínimos Quadrados , Padrões de Referência , Análise de Regressão , Reprodutibilidade dos Testes , Espectrofotometria Ultravioleta
10.
Foods ; 10(3)2021 Feb 27.
Artigo em Inglês | MEDLINE | ID: mdl-33673401

RESUMO

This study aimed to perform a systematic review and meta-analysis of the glycemic index (GI) of gluten-free bread (GFB) and its main ingredients. The systematic review followed PRISMA guidelines, using seven electronic databases (PubMed, EMBASE, Scopus, Science Direct, Web of Science, gray literature research with Google Scholar, and patents with Google Patent tool), from inception to November 2020. Eighteen studies met the inclusion criteria evaluating 132 GFB samples. Five articles tested GI in vivo, eleven in vitro; and two studies tested both methods. The analysis showed that 60.7% (95% CI: 40.2-78.1%) of the samples presented high glycemic indexes, evidencing a high glycemic profile for GFB. Only 18.2% (95% CI: 11.7-27.2%) of the bread samples presented in the studies were classified as a low GI. Meta-analysis presented moderate/low heterogenicity between studies (I2 = 61% and <1% for both high and low GIs) and reinforced the proportion of high GIs. Lower GIs were found in formulations based on Colocasia esculenta flour or enriched with fiber, yogurt and curd cheese, sourdough, psyllium, hydrocolloids, enzymes, fructans, and resistant starch, highlighting the efficacy of these ingredients to lower GFBs' GI. GFB tends to present high GI, impacting the development of chronic diseases when consumed.

11.
Molecules ; 26(3)2021 Jan 31.
Artigo em Inglês | MEDLINE | ID: mdl-33572524

RESUMO

Due to unavailability of sustainable analytical techniques for the quantitation of piperine (PPN) in food and pharmaceutical samples, there was a need to develop a rapid and sensitive sustainable analytical technique for the quantitation of PPN. Therefore, the current research presents a fast and highly sensitive normal/reversed-phase high-performance thin-layer chromatography (HPTLC) technique with classical univariate calibration for the quantitation of PPN in various food spices of black pepper with traditional (TE) and ultrasound-assisted extracts (UBE) of various food spices of Piper nigrum L. under green analytical chemistry viewpoint. The amount of PPN in TE of four different spices of black pepper-namely BPMH, BPLU, BPSH, and BPPA-was found to be 309.53, 304.97, 282.82, and 232.73 mg g-1, respectively using a sustainable normal-phase HPTLC technique. However, the amount of PPN in UBE of BPMH, BPLU, BPSH, and BPPA was recorded as 318.52, 314.60, 292.41, and 241.82 mg g-1, respectively using a sustainable normal phase HPTLC technique. The greenness of normal/reversed-phase HPTLC technique was predicted using AGREE metric approach. The eco-scale was found to be 0.90, suggested excellent greenness of normal/reversed-phase technique. UBE of PPN was also found to be superior over TE of PPN. Overall, the results of this research suggested that the proposed normal/reversed-phase densitometry technique could be effectively used for the quantitation of PPN in food and pharmaceutical samples.


Assuntos
Fracionamento Químico/métodos , Cromatografia Líquida de Alta Pressão , Cromatografia de Fase Reversa , Piper nigrum/química , Especiarias/análise , Ondas Ultrassônicas , Calibragem , Química Verde
12.
Molecules ; 26(3)2021 Jan 31.
Artigo em Inglês | MEDLINE | ID: mdl-33572688

RESUMO

The solubility values, various Hansen solubility parameters (HSPs) and thermodynamic behavior of emtricitabine (ECT) in twelve different pure solvents (PS) were estimated using various experimental as well as computational methods. Experimental solubility values (xe) of ECT in twelve different PS were obtained at T = 298.2 K to 318.2 K and p = 0.1 MPa. The xe values of ECT were correlated by "van't Hoff, Apelblat and Buchowski-Ksiazaczak λh models". Various HSPs for ECT and twelve different PS were also calculated using "HSPiP software". The xe values of ECT were estimated maximum in polyethylene glycol-400 (PEG-400; 1.41 × 10-1), followed by ethylene glycol, Transcutol-HP, propylene glycol, methanol, water, isopropanol, ethanol, 1-butanol, dimethyl sulfoxide, 2-butanol and EA (1.28 × 10-3) at T = 318.2 K. "Apparent thermodynamic analysis" showed an "endothermic and entropy-driven dissolution" of ECT. Overall, PEG-400 was found as the best/ideal solvent for solubility/miscibility of ECT compared to other solvents studied.


Assuntos
Antivirais/química , Emtricitabina/química , Solventes/química , Solubilidade , Termodinâmica
13.
Curr Pharm Des ; 27(13): 1579-1587, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33155905

RESUMO

BACKGROUND: The coronavirus disease 2019 (COVID-19) pandemic has changed the global scenario. To date, there are no treatment or preventive options. The discovery of a new drug will take time. In addition, the new drug will have side effects, and the virus will gradually become resistant to it. Therefore, it is important to search for a drug with a natural origin. OBJECTIVE: In this review, we analyzed and summarized various ethnomedicinal plants and their bioactive compounds as a source of antiviral agents for COVID-19 prevention and treatment. METHODS: From the literature, we selected different natural compounds that can act as potential targets at low cost with broad-spectrum antiviral activity. RESULTS: Of the 200 Chinese herbal extracts tested for their possible role against SARS-CoV, Lycoris radiata, Artemisia annua, Pyrrosia lingua, and Lindera aggregate showed anti-SARS-CoV effects with the median effective concentration = 2.4-88.2 µg/mL. CONCLUSION: Ethnomedicinal herbs can be used as an alternative source of novel, promising antiviral agents that might directly or indirectly inhibit the COVID-19 progression.


Assuntos
COVID-19 , Antivirais/farmacologia , Antivirais/uso terapêutico , Humanos , Pandemias , SARS-CoV-2
14.
Curr Drug Deliv ; 17(10): 824-825, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33148150
15.
Drug Deliv ; 27(1): 1625-1643, 2020 Nov 09.
Artigo em Inglês | MEDLINE | ID: mdl-33207947

RESUMO

In the last few decades, solid dispersion (SD) technology had been studied as an approach to produce an amorphous carrier to enhance the solubility, dissolution rate, and bioavailability of poorly water-soluble drugs. The use of suitable carrier and methodology in the preparation of SDs play a significant role in the biological behavior of the SDs. SDs have been prepared using a variety of pharmaceutically acceptable polymers utilizing various novel technologies. In the recent years, much attention has been paid toward the use of novel carriers and methodologies in exploring novel types of SDs to enhance therapeutic efficacy and bioavailability. The use of novel carriers and methodologies would be very beneficial for formulation scientists to develop some SDs-based formulations for their commercial use and clinical applications. In the present review, current literature of novel methodologies for SD preparation to enhance the dissolution rate, solubility, therapeutic efficacy, and bioavailability of poorly water-soluble drugs has been summarized and analyzed. Further, the current status of SDs, patent status, and future prospects have also been discussed.

16.
J Food Sci Technol ; 57(11): 4211-4219, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-33071342

RESUMO

Honey had several healing properties which includes antibacterial, anti-inflammatory and antioxidant properties. Hence, the aim of this study was to evaluate the effect of two different systems of honey on the healing of experimentally created traumatic oral ulcers in rats. Traumatic ulcers were created on the lower labial mucosa on male rats using 50% acetic acid. The rats were subsequently divided into three groups; in group one and two, the ulcers were treated with honey gel and honey adhesive respectively, whereas the third group received no treatment. The ulcers were macroscopically and microscopically studied. A statistical significant difference was observed in macroscopic investigation among the three groups in the 3rd and 7th day (p < 0.05). However, there were no statistical significant findings by the 15th day although a complete clinical healing was virtually observed in most of the cases. Histological examination shows a statistical significant difference within each of the three groups over time (p < 0.05). On the other hand, the mean rank values for the honey gel group were significantly higher in comparison to the other groups over time (p < 0.05). The therapeutic value of honey gel appears to be more effective than the mucoadhesive form in shortening the duration of wound healing.

17.
J Oleo Sci ; 69(10): 1257-1271, 2020 Oct 07.
Artigo em Inglês | MEDLINE | ID: mdl-32908093

RESUMO

This research work aimed to prepare and optimize "self-nanoemulsifying drug delivery system (SNEDDS)" by applying full factorial design (FFD) to improve solubilization and subsequently antiinflammatory efficacy of flufenamic acid (FLF). Suitable excipients were screened out based on the maximum solubility of FLF. FFD was applied using lipid (X1) and surfactant (X2) as independent variables against droplet size (Y1, nm), zeta potential (Y2, mV) and polydispersity index (PDI, Y3). Desirability function identified the main factors influencing the responses and possible interactions. Moreover, the optimized formulation (OFS1) was characterized and compared with pure FLF suspension. The prepared formulations (FS1-FS9) showed the size, PDI and zeta potential of 14.2-110.7 nm, 0.29-0.62 and -15.1 to -28.6 mV, respectively. The dispersion and emulsification of all formulations meted out within 2 min suggesting immediate release and successful solubilization. The optimized formulation OFS1 demonstrated ~ 85% drug release within 1 h which was significantly higher (p ˂ 0.05) than FLF suspension. The hemolysis study negated the probable interaction with blood cells. Eventually, improved anti-inflammatory efficacy was envisaged which might be attributed to increased drug solubility and absorption. The present nanocarrier could be a promising approach and alternative to conventional dosage form.


Assuntos
Anti-Inflamatórios/administração & dosagem , Sistemas de Liberação de Medicamentos , Emulsões , Ácido Flufenâmico/administração & dosagem , Nanopartículas , Formas de Dosagem , Composição de Medicamentos , Desenho de Fármacos , Liberação Controlada de Fármacos , Excipientes , Tamanho da Partícula , Solubilidade , Tensoativos
18.
Drug Dev Ind Pharm ; 46(10): 1716-1725, 2020 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-32893682

RESUMO

The use of bacterial ghosts (BGs) for drug delivery is an extremely fascinating perspective especially with the inherited efficient target-ability to specialized tissues. Trafficking of drug molecules across the outer membrane of Gram-negative bacteria are important to be understood for both loading (influx) and drug release (efflux). In this study, Escherichia coli (E. coli) BGs were prepared using modified protocol sponge-like reduced protocol (SLRP) which was used for loading of doxorubicin (DOX). First time in the literature, different possible factors affecting DOX loading from BGs were examined in this study. These factors including drug concentration, temperature, pH gradient, incubation time and tonicity, are proposed to effect on drug loading into E. coli BGs. Results of optimum effect from accompanied factors were found to be 10 mg/mL as DOX concentration at pH 6 with tonicity of 0.7% incubated overnight at 4 °C. After gather all factors, the amount of DOX loaded inside the BGs was recorded as 37.58%. The in vitro release studies of DOX loaded BGs over time showed a burst initial release rate of 26.75% at the first 12 h followed by a period of sustained release lasting for 16 days to give maximum release rate of 58.04%. Remarkably, DOX loaded in BG showed more apoptosis (55%) than control and DOX solution. Overall, the results indicated the presence of some important factors to be controlled when loading drugs into BGs. Also, data showed the future possibility of utilizing BGs to deliver DOX to colon cancer cells.


Assuntos
Portadores de Fármacos , Escherichia coli , Membrana Celular/metabolismo , Doxorrubicina/química , Doxorrubicina/metabolismo , Portadores de Fármacos/metabolismo , Sistemas de Liberação de Medicamentos , Liberação Controlada de Fármacos , Concentração de Íons de Hidrogênio
19.
Foods ; 9(8)2020 Aug 18.
Artigo em Inglês | MEDLINE | ID: mdl-32824752

RESUMO

Various analytical methodologies have been reported for the determination of 6-shogaol (6-SHO) and 6-gingerol (6-GIN) in ginger extracts and commercial formulations. However, green analytical methods for the determination of 6-SHO and 6-GIN, either alone or in combination, have not yet been reported in literature. Hence, the present study was aimed to develop a rapid, simple, and cheaper green reversed phase high-performance thin-layer chromatography (RP-HPTLC) densitometry method for the simultaneous determination of 6-SHO and 6-GIN in the traditional and ultrasonication-assisted extracts of ginger rhizome, commercial ginger powder, commercial capsules, and commercial ginger teas. The simultaneous analysis of 6-SHO and 6-GIN was carried out via RP-18 silica gel 60 F254S HPTLC plates. The mixture of green solvents, i.e., ethanol:water (6.5:3.5 v/v) was utilized as a mobile phase for the simultaneous analysis of 6-SHO and 6-GIN. The analysis of 6-SHO and 6-GIN was performed at λmax = 200 nm for 6-SHO and 6-GIN. The densitograms of 6-SHO and 6-GIN from traditional and ultrasonication-assisted extracts of ginger rhizome, commercial ginger powder, commercial capsules, and commercial ginger teas were verified by obtaining their single band at Rf = 0.36 ± 0.01 for 6-SHO and Rf = 0.53 ± 0.01 for 6-GIN, compared to standard 6-SHO and 6-GIN. The green RP-HPTLC method was found to be linear, in the range of 100-700 ng/band with R2 = 0.9988 for 6-SHO and 50-600 ng/band with R2 = 0.9995 for 6-GIN. In addition, the method was recorded as "accurate, precise, robust and sensitive" for the simultaneous quantification of 6-SHO and 6-GIN in traditional and ultrasonication-assisted extracts of ginger rhizome, commercial ginger powder, commercial capsules, and commercial ginger teas. The amount of 6-SHO in traditional extracts of ginger rhizome, commercial ginger powder, commercial capsules, and commercial ginger teas was obtained as 12.1, 17.9, 10.5, and 9.6 mg/g of extract, respectively. However, the amount of 6-SHO in ultrasonication-assisted extracts of ginger rhizome, commercial ginger powder, commercial capsules, and commercial ginger teas were obtained as 14.6, 19.7, 11.6, and 10.7 mg/g of extract, respectively. The amount of 6-GIN in traditional extracts of ginger rhizome, commercial ginger powder, commercial capsules, and commercial ginger teas were found as 10.2, 15.1, 7.3, and 6.9 mg/g of extract, respectively. However, the amount of 6-GIN in ultrasonication-assisted extracts of ginger rhizome, commercial ginger powder, commercial capsules, and commercial ginger teas were obtained as 12.7, 17.8, 8.8, and 7.9 mg/g of extract, respectively. Overall, the results of this study indicated that the proposed analytical technique could be effectively used for the simultaneous quantification of 6-SHO and 6-GIN in a wide range of plant extracts and commercial formulations.

20.
Pharmaceutics ; 12(8)2020 Aug 10.
Artigo em Inglês | MEDLINE | ID: mdl-32785007

RESUMO

Apigenin (APG) is a very well-known flavonoid for its anti-inflammatory and anticancer properties. The purpose of this study is to improve the solubility and bioavailability of APG using a stable bioactive self-nanoemulsifying drug delivery system (Bio-SNEDDS). APG was incorporated in an oil phase comprising coconut oil fatty acid, Imwitor 988, Transcutol P, and HCO30 to form a Bio-SNEDDS. This preparation was characterized for morphology, particle size, and transmission electron microscopy (TEM). The APG performance was investigated in terms of loading, precipitation, release and stability tests from the optimal Bio-SNEDDS. An antimicrobial test was performed to investigate the activity of the Bio-SNEDDS against the selected strains. Bioavailability of the Bio-SNEDDS was evaluated using Wister rats against the commercial oral product and the pure drug. The results demonstrated the formation of an efficient nanosized (57 nm) Bio-SNEDDS with a drug loading of 12.50 mg/gm which is around 500-fold higher than free APG. TEM analysis revealed the formation of spherical and homogeneous nanodroplets of less than 60 nm. The dissolution rate was faster than the commercial product and was able to maintain 90% APG in gastro intestinal solution for more than 4 h. A stability study demonstrated that the Bio-SNEDDS is stable at a harsh condition. The in vivo pharmacokinetics parameters of the Bio-SNEDDS formulation in comparison to the pure drug showed a significant increase in maximum concentration (Cmax) and area under the curve (AUC (0-t)) of 105.05% and 91.32%, respectively. Moreover, the antimicrobial study revealed moderate inhibition in the bacterial growth rate. The APG-Bio-SNEDDS could serve as potential carrier aimed at improving the clinical application of APG.

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