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Dettagli della rivista
Formato
Rivista
eISSN
1846-9558
ISSN
1330-0075
Pubblicato per la prima volta
28 Feb 2007
Periodo di pubblicazione
4 volte all'anno
Lingue
Inglese

Cerca

Volume 63 (2013): Edizione 4 (December 2013)

Dettagli della rivista
Formato
Rivista
eISSN
1846-9558
ISSN
1330-0075
Pubblicato per la prima volta
28 Feb 2007
Periodo di pubblicazione
4 volte all'anno
Lingue
Inglese

Cerca

10 Articoli
Accesso libero

Lipid-based systems as a promising approach for enhancing the bioavailability of poorly water-soluble drugs

Pubblicato online: 31 Dec 2013
Pagine: 427 - 445

Astratto

Abstract

Low oral bioavailability as a consequence of low water solubility of drugs is a growing challenge to the development of new pharmaceutical products. One of the most popular approaches of oral bioavailability and solubility enhancement is the utilization of lipid-based drug delivery systems. Their use in product development is growing due to the versatility of pharmaceutical lipid excipients and drug formulations, and their compatibility with liquid, semi-solid, and solid dosage forms. Lipid formulations, such as self-emulsifying (SEDDS), self-microemulsifying SMEDDS) and self- -nanoemulsifying drug delivery systems (SNEDDS) were explored in many studies as an efficient approach for improving the bioavailability and dissolution rate of poorly water-soluble drugs. One of the greatest advantages of incorporating poorly soluble drugs into such formulations is their spontaneous emulsification and formation of an emulsion, microemulsion or nanoemulsion in aqueous media. This review article focuses on the following topics. First, it presents a classification overview of lipid-based drug delivery systems and mechanisms involved in improving the solubility and bioavailability of poorly water-soluble drugs. Second, the article reviews components of lipid-based drug delivery systems for oral use with their characteristics. Third, it brings a detailed description of SEDDS, SMEDDS and SNEDDS, which are very often misused in literature, with special emphasis on the comparison between microemulsions and nanoemulsions.

Parole chiave

  • lipid-based drug delivery systems (LBDDS)
  • self-emulsifying drug delivery systems (SEDDS)
  • self-microemulsifying drug delivery systems (SMEDDS)
  • self-nanoemulsifying drug delivery systems (SNEDDS)
  • microemulsions
  • nanoemulsions
Accesso libero

Liquisolid systems and aspects influencing their research and development

Pubblicato online: 31 Dec 2013
Pagine: 447 - 465

Astratto

Abstract

Many modern drugs are poorly water soluble substances, which causes difficulties in the development of solid dosage forms with sufficient bioavailability. Preparation of liquisolid systems (LSS) is a novel technique for improving solubility, dissolution and bioavailability of such drugs. The basic principle of LSS preparation is conversion of the drug in liquid state into a free-flowing, compressible, dry powder through its absorption into suitable excipients - porous carriers (aluminometasilicates, microcrystalline cellulose), subsequently coated with material having high absorption capacity (silicon dioxide commonly known as colloidal silica). LSS exhibit advantages such as lower production costs compared to soft capsules, simple processing and enhanced drug release. The main benefit is higher bioavailability of the liquid drug, caused by a large surface area available for absorption. The article tries to clarify specific aspects connected with the formulation of LSS: properties of excipients (surface area, absorption capacity), variables related to the processing (solubility, liquid load factor) and dosage form evaluation.

Parole chiave

  • bioavailability improvement
  • carrier material
  • enhanced release
  • liquid drug
  • liquisolid technology
Accesso libero

An in vitro based investigation into the cytotoxic effects of D-amino acids

Pubblicato online: 31 Dec 2013
Pagine: 467 - 478

Astratto

Abstract

In the present study, cytotoxic effects of D-Ala, D-Pro and D-Lys are demonstrated. In an effort to study the possible mechanisms of the observed cytotoxicity, catalase activity, H2O2 generation, and apoptotic activity were measured in HeLa and MCF-7 cell lines. Although D-Lys is a poor substrate for DAO and therefore low H2O2 was detected, it was shown to provoke severe impairment of cellular integrity and survival. Interestingly, a very good substrate for DAO, such as D-Pro, did not substantially reduce cell viability. On the other hand, a moderate substrate for DAO, represented by D-Ala, was shown to moderately trigger toxicity in the tested cell lines. Although a correlation between the in vitro cytotoxicity of D-amino acids and the amount of H2O2 produced was absent, there was a good agreement between the ability of D-amino acids to trigger apoptosis and to provoke toxicity. Our results indicate that the toxicity of D-amino acids does not appear to be solely mediated by H2O2. Therefore, we hypothesize that other possible contributing apoptosis-mediated pathways might cause the observed toxicity.

Parole chiave

  • D-amino acids
  • toxicity
  • HeLa cells
  • MCF7 cells
  • catalase
  • apoptosis
  • oxidative stress
Accesso libero

Preparation and evaluation of chitosan based thermoreversible gels for intraperitoneal delivery of 5-fluorouracil (5-FU)

Pubblicato online: 31 Dec 2013
Pagine: 479 - 491

Astratto

Abstract

Sterile thermoreversibly gelling systems based on chitosan- glycerol phosphate were developed for intraperitoneal delivery of the antineoplastic agent 5-FU. The formulation was evaluated for gelling characteristics and in vitro drug release. Drug free gels were evaluated for in vitro cytotoxicity in L-929 mouse fibroblast cells. Drug loaded gels were subjected to acute toxicity studies in Swiss albino mice via intraperitoneal route and efficacy studies via intratumoral injections in subcutaneous colon carcinoma bearing BALB/c mice. The formulations gelled reversibly in 8 min at 37 °C and provided prolonged release of the drug. Drug free systems showed dose dependent cytotoxicity in fibroblast cells, while in vivo studies revealed a 2.8-fold increase in LD50 of 5-FU administered intraperitoneally as the developed system. Tumor volume measurements showed comparable efficacy of 5-FU administered as gel and commercial injection with a greatly improved safety profile of the former as adjudged from mortality and body weight measurements.

Parole chiave

  • chitosan
  • glycerophosphate
  • thermoreversible gels
  • intraperitoneal
  • 5-fluorouracil
Accesso libero

Cytoprotective potential of anti-ischemic drugs against chemotherapy-induced cardiotoxicity in H9c2 myoblast cell line

Pubblicato online: 31 Dec 2013
Pagine: 493 - 503

Astratto

Abstract

To investigate potential prevention or attenuation of anti- cancer drug induced cardiotoxicity using anti-ischemic drugs, a rat myoblast (H9c2) cell line was used as our in vitro cardiac model. Irinotecan and doxorubicin were found to be cytotoxic for the H9c2 cell line with IC50 of 30.69 ± 6.20 and 20.94 ± 6.05 mmol L-1, respectively. 5-Flurouracil and cladribine were not cytotoxic and thus IC50 could not be calculated. When 100 mmol L-1 doxorubicin was incubated for 72 hours with 50 mmol L-1 diltiazem, 100 mmol L-1 dexrazoxane and 100 mmol L-1 losartan, respectively, there was a 58.7 ± 10.2, 52.2 ± 11.7 and 44.7 ± 5.4 % reduction in cell death. When 200 mmol L-1 irinotecan was incubated for 72 hours with 100 mmol L-1 dexrazoxane, losartan and diltiazem, respectively, a 27.7 ± 6.9, 25.6 ± 5.1, and 19.1 ± 2.3 % reduction in cell death was observed. Our data suggests that losartan and diltiazem were as effective as dexrazoxane in protecting the cells against irinotecan- and doxorubicin-induced cell toxicity. These findings offer potential uses of anti- -ischemic drugs for ablation of cytotoxicity in response to mitochondrial injury, thereby improving patient outcomes and reducing health-care costs.

Parole chiave

  • rat myoblast (H9c2)
  • cytoprotection
  • dexrazoxane
  • doxorubicin
  • diltiazem
  • irinotecan
Accesso libero

Chemical fingerprinting and quantitative analysis of two common Gleditsia sinensis fruits using HPLC-DAD

Pubblicato online: 31 Dec 2013
Pagine: 505 - 515

Astratto

Abstract

Gleditsiae Fructus Abnormalis and Gleditsiae Sinensis Fructus are obtained from different developmental stages of fruits from Gleditsia sinensis Lam. (Leguminosae). The possible interchangeable usage of the two fruits, however, has long been very controversial. Here, high performance liquid chromatography coupled with diode array detection was developed to explore their chemical fingerprinting profiles. Besides, the amounts of aglycones of saponin compounds, echinocystic acid and oleanolic acid in both fruits were quantified. The results indicated that there was no significant difference in the content of aglycones from the two types of fruits. However, their chromatographic fingerprints showed distinct characteristics. Therefore, the interchangeable application of these fruits has to be taken with a specific precaution.

Parole chiave

  • Gleditsiae Fructus Abnormalis
  • Gleditsiae Sinensis Fructus
  • HPLC-DAD
  • fingerprinting
Accesso libero

Development and evaluation of coenzyme Q10 loaded solid lipid nanoparticle hydrogel for enhanced dermal delivery

Pubblicato online: 31 Dec 2013
Pagine: 517 - 529

Astratto

Abstract

Coenzyme Q10 (Q10) loaded solid lipid nanoparticles (SLN) were prepared by the high speed homogenization method and incorporated into Carbopol 974P hydrogels. Compritol 888 ATO (C888) was employed as the lipid base; Poloxamer 188 (P188) and Tween 80 (Tw80) were used as surfactant and co-surfactant. Optimum particle size with narrow distribution was obtained as 152.2 nm for blank and 142.4 nm for Q10 loaded SLNs. The overall charge of loaded SLNs was -13.7 ± 1.3 mV. Q10 entrapment efficiency was 89 % and the production yield was 94 %. Transmission electron microscopy analysis provided evidence of colloidal size, spherical shape while differential scanning calorimetry analysis confirmed recrystallization of the lipid after the preparation of SLNs. Trolox equivalent antioxidant capacity (TEAC) analysis has shown that antioxidant potential of Q10 can be protected in SLNs. Rheological characteristics demonstrated that the SLN incorporating gels were shear thinning and the mechanical strength of the gels was suitable for topical application. Diffusion studies from rat abdominal skin revealed that the delivery of Q10 was doubled in SLN incorporating gels, approximately 40 μg cm-2, in comparison with gels prepared with only Q10 (not incorporated in SLNs). As a result, it can be stated that Q10-SLN loaded gels can be successful delivery systems for carrying Q10 efficiently into the skin without losing its antioxidant properties.

Parole chiave

  • antioxidant
  • coenzyme Q10
  • skin delivery
  • hydrogel
  • solid lipid nanoparticles
Accesso libero

Design and in vivo evaluation of emulgel formulations including green tea extract and rose oil

Pubblicato online: 31 Dec 2013
Pagine: 531 - 544

Astratto

Abstract

Prevention of skin aging and its treatment is an emerging field for development of new formulations in cosmetics. Accordingly, plant extracts with antioxidant properties are beneficial cosmetic ingredients for this purpose. This study was aimed at developing a stable and easily manufactured emulgel including green tea extract and rose oil that is effective on the barrier function and hydration of the skin. An emulgel formulation containing 20 % green tea extract and 5 % rose oil was designed as a result of pre-formulation studies. Physicochemical characterization, in vitro stability studies, in vivo water content of the stratum corneum and transepidermal water loss studies were carried out afterwards. In vivo studies on ten female subjects were evaluated by using non-invasive skin bioengineering techniques. Finally, a cosmetically acceptable, stable and effective emulgel formulation for skin barrier function with good hydrating properties was obtained for skin hydration, protection and anti-aging purposes.

Parole chiave

  • green tea extract
  • rose oil
  • emulgel
  • skin water content
  • transepidermal water loss
  • biophysical measurements
Accesso libero

In vitro dissolution and in vivo gamma scintigraphic evaluation of press-coated salbutamol sulfate tablets

Pubblicato online: 31 Dec 2013
Pagine: 545 - 551

Astratto

Abstract

The aim of this study was to investigate the in vitro and in vivo performance of salbutamol sulfate press-coated tablets for delayed release. The in vitro release behavior of press-coated tablets with the outer layer of PEG 6000/ Eudragit S100 blends (2:1) in pH 1.2 (0.1 mol L-1 HCl) and then pH 6.8 buffer solution was examined. Morphological change of the press-coated tablet during in vitro release was recorded with a digital camera. Release of salbutamol sulfate from press-coated tablets was less than 5 % before 3 h and was completed after 8 h in pH 6.8 phosphate buffer solution. In vivo gamma scintigraphy study carried out on healthy men indicated that the designed system released the drug in lower parts of the GI tract after a lag time of 5 hours. The results showed the capability of the system of achieving delayed release of the drug in both in vitro and in vivo gamma scintigraphy studies.

Parole chiave

  • salbutamol sulfate
  • press-coated tablet
  • PEG 6000-Eudragit S100 blends
  • dissolution
  • gamma scintigraphy
Accesso libero

The content of fagopyrin and polyphenols in common and tartary buckwheat sprouts

Pubblicato online: 31 Dec 2013
Pagine: 553 - 560

Astratto

Abstract

Dried buckwheat herb is used in medicinal products whereas fresh green plant parts, especially sprouts, are consumed as a vegetable. The herb contains fagopyrins, which cause sensitivity to light after ingestion. The aim of this study was to investigate the impact of different growing conditions and the development phase on the content of fagopyrin and phenolic compounds in buckwheat sprouts. Total flavonoid and total phenol contents, fagopyrin content and antioxidant activity were determined spectrophotometrically. Fagopyrin and flavonoids were located almost exclusively in cotyledons. Based on a comparison to hypericin toxicity, the recommendable intake of buckwheat sprouts was estimated to be less than 40 g per day.

Parole chiave

  • buckwheat
  • Fagopyrum (Polygonaceae)
  • fagopyrin
  • polyphenols
  • sprouts
  • phototoxicity
10 Articoli
Accesso libero

Lipid-based systems as a promising approach for enhancing the bioavailability of poorly water-soluble drugs

Pubblicato online: 31 Dec 2013
Pagine: 427 - 445

Astratto

Abstract

Low oral bioavailability as a consequence of low water solubility of drugs is a growing challenge to the development of new pharmaceutical products. One of the most popular approaches of oral bioavailability and solubility enhancement is the utilization of lipid-based drug delivery systems. Their use in product development is growing due to the versatility of pharmaceutical lipid excipients and drug formulations, and their compatibility with liquid, semi-solid, and solid dosage forms. Lipid formulations, such as self-emulsifying (SEDDS), self-microemulsifying SMEDDS) and self- -nanoemulsifying drug delivery systems (SNEDDS) were explored in many studies as an efficient approach for improving the bioavailability and dissolution rate of poorly water-soluble drugs. One of the greatest advantages of incorporating poorly soluble drugs into such formulations is their spontaneous emulsification and formation of an emulsion, microemulsion or nanoemulsion in aqueous media. This review article focuses on the following topics. First, it presents a classification overview of lipid-based drug delivery systems and mechanisms involved in improving the solubility and bioavailability of poorly water-soluble drugs. Second, the article reviews components of lipid-based drug delivery systems for oral use with their characteristics. Third, it brings a detailed description of SEDDS, SMEDDS and SNEDDS, which are very often misused in literature, with special emphasis on the comparison between microemulsions and nanoemulsions.

Parole chiave

  • lipid-based drug delivery systems (LBDDS)
  • self-emulsifying drug delivery systems (SEDDS)
  • self-microemulsifying drug delivery systems (SMEDDS)
  • self-nanoemulsifying drug delivery systems (SNEDDS)
  • microemulsions
  • nanoemulsions
Accesso libero

Liquisolid systems and aspects influencing their research and development

Pubblicato online: 31 Dec 2013
Pagine: 447 - 465

Astratto

Abstract

Many modern drugs are poorly water soluble substances, which causes difficulties in the development of solid dosage forms with sufficient bioavailability. Preparation of liquisolid systems (LSS) is a novel technique for improving solubility, dissolution and bioavailability of such drugs. The basic principle of LSS preparation is conversion of the drug in liquid state into a free-flowing, compressible, dry powder through its absorption into suitable excipients - porous carriers (aluminometasilicates, microcrystalline cellulose), subsequently coated with material having high absorption capacity (silicon dioxide commonly known as colloidal silica). LSS exhibit advantages such as lower production costs compared to soft capsules, simple processing and enhanced drug release. The main benefit is higher bioavailability of the liquid drug, caused by a large surface area available for absorption. The article tries to clarify specific aspects connected with the formulation of LSS: properties of excipients (surface area, absorption capacity), variables related to the processing (solubility, liquid load factor) and dosage form evaluation.

Parole chiave

  • bioavailability improvement
  • carrier material
  • enhanced release
  • liquid drug
  • liquisolid technology
Accesso libero

An in vitro based investigation into the cytotoxic effects of D-amino acids

Pubblicato online: 31 Dec 2013
Pagine: 467 - 478

Astratto

Abstract

In the present study, cytotoxic effects of D-Ala, D-Pro and D-Lys are demonstrated. In an effort to study the possible mechanisms of the observed cytotoxicity, catalase activity, H2O2 generation, and apoptotic activity were measured in HeLa and MCF-7 cell lines. Although D-Lys is a poor substrate for DAO and therefore low H2O2 was detected, it was shown to provoke severe impairment of cellular integrity and survival. Interestingly, a very good substrate for DAO, such as D-Pro, did not substantially reduce cell viability. On the other hand, a moderate substrate for DAO, represented by D-Ala, was shown to moderately trigger toxicity in the tested cell lines. Although a correlation between the in vitro cytotoxicity of D-amino acids and the amount of H2O2 produced was absent, there was a good agreement between the ability of D-amino acids to trigger apoptosis and to provoke toxicity. Our results indicate that the toxicity of D-amino acids does not appear to be solely mediated by H2O2. Therefore, we hypothesize that other possible contributing apoptosis-mediated pathways might cause the observed toxicity.

Parole chiave

  • D-amino acids
  • toxicity
  • HeLa cells
  • MCF7 cells
  • catalase
  • apoptosis
  • oxidative stress
Accesso libero

Preparation and evaluation of chitosan based thermoreversible gels for intraperitoneal delivery of 5-fluorouracil (5-FU)

Pubblicato online: 31 Dec 2013
Pagine: 479 - 491

Astratto

Abstract

Sterile thermoreversibly gelling systems based on chitosan- glycerol phosphate were developed for intraperitoneal delivery of the antineoplastic agent 5-FU. The formulation was evaluated for gelling characteristics and in vitro drug release. Drug free gels were evaluated for in vitro cytotoxicity in L-929 mouse fibroblast cells. Drug loaded gels were subjected to acute toxicity studies in Swiss albino mice via intraperitoneal route and efficacy studies via intratumoral injections in subcutaneous colon carcinoma bearing BALB/c mice. The formulations gelled reversibly in 8 min at 37 °C and provided prolonged release of the drug. Drug free systems showed dose dependent cytotoxicity in fibroblast cells, while in vivo studies revealed a 2.8-fold increase in LD50 of 5-FU administered intraperitoneally as the developed system. Tumor volume measurements showed comparable efficacy of 5-FU administered as gel and commercial injection with a greatly improved safety profile of the former as adjudged from mortality and body weight measurements.

Parole chiave

  • chitosan
  • glycerophosphate
  • thermoreversible gels
  • intraperitoneal
  • 5-fluorouracil
Accesso libero

Cytoprotective potential of anti-ischemic drugs against chemotherapy-induced cardiotoxicity in H9c2 myoblast cell line

Pubblicato online: 31 Dec 2013
Pagine: 493 - 503

Astratto

Abstract

To investigate potential prevention or attenuation of anti- cancer drug induced cardiotoxicity using anti-ischemic drugs, a rat myoblast (H9c2) cell line was used as our in vitro cardiac model. Irinotecan and doxorubicin were found to be cytotoxic for the H9c2 cell line with IC50 of 30.69 ± 6.20 and 20.94 ± 6.05 mmol L-1, respectively. 5-Flurouracil and cladribine were not cytotoxic and thus IC50 could not be calculated. When 100 mmol L-1 doxorubicin was incubated for 72 hours with 50 mmol L-1 diltiazem, 100 mmol L-1 dexrazoxane and 100 mmol L-1 losartan, respectively, there was a 58.7 ± 10.2, 52.2 ± 11.7 and 44.7 ± 5.4 % reduction in cell death. When 200 mmol L-1 irinotecan was incubated for 72 hours with 100 mmol L-1 dexrazoxane, losartan and diltiazem, respectively, a 27.7 ± 6.9, 25.6 ± 5.1, and 19.1 ± 2.3 % reduction in cell death was observed. Our data suggests that losartan and diltiazem were as effective as dexrazoxane in protecting the cells against irinotecan- and doxorubicin-induced cell toxicity. These findings offer potential uses of anti- -ischemic drugs for ablation of cytotoxicity in response to mitochondrial injury, thereby improving patient outcomes and reducing health-care costs.

Parole chiave

  • rat myoblast (H9c2)
  • cytoprotection
  • dexrazoxane
  • doxorubicin
  • diltiazem
  • irinotecan
Accesso libero

Chemical fingerprinting and quantitative analysis of two common Gleditsia sinensis fruits using HPLC-DAD

Pubblicato online: 31 Dec 2013
Pagine: 505 - 515

Astratto

Abstract

Gleditsiae Fructus Abnormalis and Gleditsiae Sinensis Fructus are obtained from different developmental stages of fruits from Gleditsia sinensis Lam. (Leguminosae). The possible interchangeable usage of the two fruits, however, has long been very controversial. Here, high performance liquid chromatography coupled with diode array detection was developed to explore their chemical fingerprinting profiles. Besides, the amounts of aglycones of saponin compounds, echinocystic acid and oleanolic acid in both fruits were quantified. The results indicated that there was no significant difference in the content of aglycones from the two types of fruits. However, their chromatographic fingerprints showed distinct characteristics. Therefore, the interchangeable application of these fruits has to be taken with a specific precaution.

Parole chiave

  • Gleditsiae Fructus Abnormalis
  • Gleditsiae Sinensis Fructus
  • HPLC-DAD
  • fingerprinting
Accesso libero

Development and evaluation of coenzyme Q10 loaded solid lipid nanoparticle hydrogel for enhanced dermal delivery

Pubblicato online: 31 Dec 2013
Pagine: 517 - 529

Astratto

Abstract

Coenzyme Q10 (Q10) loaded solid lipid nanoparticles (SLN) were prepared by the high speed homogenization method and incorporated into Carbopol 974P hydrogels. Compritol 888 ATO (C888) was employed as the lipid base; Poloxamer 188 (P188) and Tween 80 (Tw80) were used as surfactant and co-surfactant. Optimum particle size with narrow distribution was obtained as 152.2 nm for blank and 142.4 nm for Q10 loaded SLNs. The overall charge of loaded SLNs was -13.7 ± 1.3 mV. Q10 entrapment efficiency was 89 % and the production yield was 94 %. Transmission electron microscopy analysis provided evidence of colloidal size, spherical shape while differential scanning calorimetry analysis confirmed recrystallization of the lipid after the preparation of SLNs. Trolox equivalent antioxidant capacity (TEAC) analysis has shown that antioxidant potential of Q10 can be protected in SLNs. Rheological characteristics demonstrated that the SLN incorporating gels were shear thinning and the mechanical strength of the gels was suitable for topical application. Diffusion studies from rat abdominal skin revealed that the delivery of Q10 was doubled in SLN incorporating gels, approximately 40 μg cm-2, in comparison with gels prepared with only Q10 (not incorporated in SLNs). As a result, it can be stated that Q10-SLN loaded gels can be successful delivery systems for carrying Q10 efficiently into the skin without losing its antioxidant properties.

Parole chiave

  • antioxidant
  • coenzyme Q10
  • skin delivery
  • hydrogel
  • solid lipid nanoparticles
Accesso libero

Design and in vivo evaluation of emulgel formulations including green tea extract and rose oil

Pubblicato online: 31 Dec 2013
Pagine: 531 - 544

Astratto

Abstract

Prevention of skin aging and its treatment is an emerging field for development of new formulations in cosmetics. Accordingly, plant extracts with antioxidant properties are beneficial cosmetic ingredients for this purpose. This study was aimed at developing a stable and easily manufactured emulgel including green tea extract and rose oil that is effective on the barrier function and hydration of the skin. An emulgel formulation containing 20 % green tea extract and 5 % rose oil was designed as a result of pre-formulation studies. Physicochemical characterization, in vitro stability studies, in vivo water content of the stratum corneum and transepidermal water loss studies were carried out afterwards. In vivo studies on ten female subjects were evaluated by using non-invasive skin bioengineering techniques. Finally, a cosmetically acceptable, stable and effective emulgel formulation for skin barrier function with good hydrating properties was obtained for skin hydration, protection and anti-aging purposes.

Parole chiave

  • green tea extract
  • rose oil
  • emulgel
  • skin water content
  • transepidermal water loss
  • biophysical measurements
Accesso libero

In vitro dissolution and in vivo gamma scintigraphic evaluation of press-coated salbutamol sulfate tablets

Pubblicato online: 31 Dec 2013
Pagine: 545 - 551

Astratto

Abstract

The aim of this study was to investigate the in vitro and in vivo performance of salbutamol sulfate press-coated tablets for delayed release. The in vitro release behavior of press-coated tablets with the outer layer of PEG 6000/ Eudragit S100 blends (2:1) in pH 1.2 (0.1 mol L-1 HCl) and then pH 6.8 buffer solution was examined. Morphological change of the press-coated tablet during in vitro release was recorded with a digital camera. Release of salbutamol sulfate from press-coated tablets was less than 5 % before 3 h and was completed after 8 h in pH 6.8 phosphate buffer solution. In vivo gamma scintigraphy study carried out on healthy men indicated that the designed system released the drug in lower parts of the GI tract after a lag time of 5 hours. The results showed the capability of the system of achieving delayed release of the drug in both in vitro and in vivo gamma scintigraphy studies.

Parole chiave

  • salbutamol sulfate
  • press-coated tablet
  • PEG 6000-Eudragit S100 blends
  • dissolution
  • gamma scintigraphy
Accesso libero

The content of fagopyrin and polyphenols in common and tartary buckwheat sprouts

Pubblicato online: 31 Dec 2013
Pagine: 553 - 560

Astratto

Abstract

Dried buckwheat herb is used in medicinal products whereas fresh green plant parts, especially sprouts, are consumed as a vegetable. The herb contains fagopyrins, which cause sensitivity to light after ingestion. The aim of this study was to investigate the impact of different growing conditions and the development phase on the content of fagopyrin and phenolic compounds in buckwheat sprouts. Total flavonoid and total phenol contents, fagopyrin content and antioxidant activity were determined spectrophotometrically. Fagopyrin and flavonoids were located almost exclusively in cotyledons. Based on a comparison to hypericin toxicity, the recommendable intake of buckwheat sprouts was estimated to be less than 40 g per day.

Parole chiave

  • buckwheat
  • Fagopyrum (Polygonaceae)
  • fagopyrin
  • polyphenols
  • sprouts
  • phototoxicity

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