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1.
Molecules ; 26(4)2021 Feb 19.
Artigo em Inglês | MEDLINE | ID: mdl-33669650

RESUMO

Apples are an important source of biologically active compounds. Consequently, we decided to model hard gelatin capsules with lyophilized apple powder by using different excipients and to evaluate the release kinetics of phenolic compounds. The apple slices of "Ligol" cultivar were immediately frozen in a freezer (at -35°C) with air circulation and were lyophilized with a sublimator at the pressure of 0.01 mbar (condenser temperature, -85°C). Lyophilized apple powder was used as an active substance filled into hard gelatin capsules. We conducted capsule disintegration and dissolution tests to evaluate the quality of apple lyophilizate-containing capsules of different encapsulating content. Individual phenolic compounds can be arranged in the following descending order according to the amount released from the capsules of different compositions: chlorogenic acid > rutin > avicularin > hyperoside > phloridzin > quercitrin > (-)-epicatechin > isoquercitrin. Chlorogenic acid was the compound that was released in the highest amounts from capsules of different encapsulating content: its released amounts ranged from 68.4 to 640.3 µg/mL. According to the obtained data, when hypromellose content ranged from 29% to 41% of the capsule mass, the capsules disintegrated within less than 30 min, and such amounts of hypromellose did not prolong the release of phenolic compounds. Based on the results of the dissolution test, the capsules can be classified as fast-dissolving preparations, as more than 85% of the active substances were released within 30 min.


Assuntos
Produtos Biológicos/análise , Cápsulas/química , Liofilização , Malus/química , Etanol/química , Gelatina/química , Glicosídeos/química , Fenóis/análise , Fenóis/química , Pós
2.
Molecules ; 26(12)2021 Jun 10.
Artigo em Inglês | MEDLINE | ID: mdl-34200887

RESUMO

Royal jelly is a natural substance produced by worker bees that possesses a variety of biological activities, including antioxidant, anti-inflammatory, antibacterial, and protective. Although fresh royal jelly is kept at low temperatures, to increase its stability, it needs to be incorporated into pharmaceutical formulations, such as in situ gels. The aim of this study was to formulate in situ ocular gels containing Lithuanian royal jelly for topical corneal use in order to increase the retention time of the formulation on the ocular surface and bioavailability. Gels were evaluated for physicochemical characteristics (pH, rheological properties, refractive index) and in vitro drug release measuring the amount of 10-hydroxy-2-decenoic acid (10-HDA). An ocular irritation test and cell viability tests were performed using the SIRC (Statens Seruminstitut Rabbit Cornea) cell culture line. Results indicated that all the in situ gels were within an acceptable pH and refractive index range close to corneal properties. Rheology studies have shown that the gelation temperature varies between 25 and 32 °C, depending on the amount of poloxamers. The release studies have shown that the release of 10-HDA from in situ gels is more sustained than royal jelly suspension. All gel formulations were non-irritant according to the short-time exposure test (STE) using the SIRC cell culture line, and long-term cell viability studies indicated that the formulations used in small concentrations did not induce cell death. Prepared in situ gels containing royal jelly have potential for ocular drug delivery, and they may improve the bioavailability, stability of royal jelly, and formation of non-irritant ocular formulations.


Assuntos
Córnea/efeitos dos fármacos , Ácidos Graxos/química , Ácidos Graxos/farmacologia , Géis/química , Géis/farmacologia , Animais , Abelhas/metabolismo , Disponibilidade Biológica , Produtos Biológicos/química , Produtos Biológicos/farmacocinética , Produtos Biológicos/farmacologia , Morte Celular/efeitos dos fármacos , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Química Farmacêutica/métodos , Córnea/metabolismo , Ácidos Decanoicos/química , Preparações de Ação Retardada/química , Preparações de Ação Retardada/farmacocinética , Preparações de Ação Retardada/farmacologia , Sistemas de Liberação de Medicamentos/métodos , Liberação Controlada de Fármacos/efeitos dos fármacos , Excipientes/química , Géis/farmacocinética , Poloxâmero/química , Coelhos , Reologia , Temperatura
3.
Acta Pol Pharm ; 74(2): 543-549, 2017 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-29624259

RESUMO

The ciclopirox olamine (CPO) has a broad antimicrobial profile including dermatophytes, yeasts and is used in various pharmaceutical forms. The aim of this study is to evaluate the quality of the CPO gels according to biopharmaceutial tests in vitro and antifungal activity assay. Hydroxypropyl cellulose, chitosan and poloxamer 407 were selected as agents gelificants. The effects of gelling agent properties and concentration on the consistency and flow characteristics have been studied by rheometer. CPO release rates from gel were measured with Franz type diffusion cells. The antifungal activity of gels was tested using agar well diffusion technique. The results of the experimental study have shown that the rheological properties of the medications depend on the selected gelling agent and the amount of it. The higher amounts of CPO were released from the poloxamer 407 gels. Though all tested CPO gels showed great inhibition of Microsporn canis.


Assuntos
Antifúngicos/química , Piridonas/química , Tecnologia Farmacêutica/métodos , Antifúngicos/farmacologia , Biofarmácia , Celulose/análogos & derivados , Celulose/química , Química Farmacêutica , Quitosana , Ciclopirox , Testes de Sensibilidade a Antimicrobianos por Disco-Difusão , Composição de Medicamentos , Liberação Controlada de Fármacos , Géis , Cinética , Microsporum/efeitos dos fármacos , Microsporum/crescimento & desenvolvimento , Modelos Químicos , Poloxâmero/química , Piridonas/farmacologia , Reologia , Solubilidade , Viscosidade
4.
Acta Pol Pharm ; 73(4): 955-965, 2016 07.
Artigo em Inglês | MEDLINE | ID: mdl-29648721

RESUMO

There is a great potential for a semi-solid preparation for topical application to the skin that would use materials of natural origin not only as an active substance but also as its base. The aim of this research was to model semisolid preparations containing hawthorn extract and to determine the effect of their bases (carriers) on the release of active components from experimental dosage forms, based on the results of the in vitro studies of the bioactivity of hawthorn active components and ex vivo skin penetration studies. The active compounds of hawthorn were indentified and quantified by validated HPLC method. The antimicrobial and anti-radical activity of dry hawthorn extract were evaluated by methods in vitro. The penetration of active substances into the full undamaged human skin was evaluated by method ex vivo. Natural topical composition was chosen according to the results of release of active compounds. Release experiments were performed with modified Franz type diffusion cells. B.ceieus was the most sensitive bacteria for the hawthorn extract. Extract showed antiradical activity, however the penetration was limited. Only traces of hyperoside and isoquercitrin were founded in epidermis. Protective topical preparation with shea butter released 41.4-42.4% of active substances. Four major compounds of dry hawthorn extract were identified. The research showed that extract had antimicrobial and antiradical activity, however compounds of hawthorn stay on the surface of the undamaged human skin. Topical preparation containing beeswax did not release active compounds. Beeswax was identified as suspending agent. Topical preparations released active compounds when shea butter was used instead of beeswax.


Assuntos
Crataegus , Extratos Vegetais/farmacologia , Administração Tópica , Anti-Infecciosos/farmacologia , Cromatografia Líquida de Alta Pressão , Crataegus/química , Sequestradores de Radicais Livres/farmacologia , Humanos , Extratos Vegetais/farmacocinética , Pele/metabolismo , Ceras
5.
Acta Pol Pharm ; 73(1): 153-61, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27008810

RESUMO

Scientific literature provides a great deal of studies supporting antioxidant effects of rosemary, protecting the body's cells against reactive oxygen species and their negative impact. Ethanol rosemary extracts were produced by maceration method. To assess biological activity of rosemary extracts, antioxidant and antimicrobial activity tests were performed. Antimicrobial activity tests revealed that G+ microorganisms are most sensitive to liquid rosemary extract, while G-microorganisms are most resistant to it. For the purposes of experimenting, five types of semisolid systems were modeled: hydrogel, oleogel, absorption-hydrophobic ointment, oil-in-water-type cream and water-in-oil-type cream, which contained rosemary extract as an active ingredient. Study results show that liquid rosemary extract was distributed evenly in the aqueous phase of water-in-oil-type system, forming the stable emulsion systems. The following research aim was chosen to evaluate the semisolid systems with rosemary exctract: to model semisolid preparations with liquid rosemary extract and determine the influence of excipients on their quality, and perform in vitro study of the release of active ingredients and antimicrobial activity. It was found that oil-in-water type gel-cream has antimicrobial activity against Staphylococcus epidermidis bacteria and Candida albicans fungus, while hydrogel affected only Candida albicans. According to the results of biopharmaceutical study, modeled semisolid systems with rosemary extract can be arranged in an ascending order of the release of phenolic compounds from the forms: water-in-oil-type cream < absorption-hydrophobic ointment < Pionier PLW oleogel < oil-in-water-type eucerin cream < hydrogel < oil-in-water-type gel-cream. Study results showed that oil-in-water-type gel-cream is the most suitable vehicle for liquid rosemary extract used as an active ingredient.


Assuntos
Anti-Infecciosos/química , Extratos Vegetais/química , Rosmarinus/química , Anti-Infecciosos/farmacologia , Biofarmácia , Géis , Pomadas , Extratos Vegetais/análise , Extratos Vegetais/farmacologia
6.
Acta Pol Pharm ; 73(6): 1623-1630, 2016 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-29634118

RESUMO

Many researchers have advocated in recent times that antiseptic use in healing wounds should be discouraged. Antiseptics have been found to retard healing of wounds. Poloxamer 407 shows thermoreversible properties, which are of the utmost interest in optimizing drug formulation (fluid state at room temperature facilitating administration and gel state above sol-gel transition temperature, at body temperature, promoting prolonged release of pharmacological agents). Chlorhexidine, a commonly used antiseptic, is known to be less toxic on granulation cells. Acting as an antiseptic, it is an effective bactericidal agent against the most categories of microbes, including bacteria, yeast, and viruses. Objective of this study was to evaluate antimicrobial activ- ity of chlorhexidine containing poloxamer gel to Gram-positive and Gram-negative bacteria in vitro. Chlorhexidine gels and chlorhexidine aqueous solutions have different antibacterial activity to S. amis, E.faecalis, E. coli and P. aemginosa strains in vitro. It depends on concentration and dosage form of antiseptic. Study results confirmed that antimicrobial activity of gel depends on active ingredient concentration in antiseptic. The best inhibition effect for both of reference and wild-type bacteria was obtained for 1% chlorhexidine gel. Summarizing the results and assessing the characteristics of the gel ingredients, it can be suggested using chlorhexidine gels in veterinary medicine.


Assuntos
Antibacterianos/farmacologia , Clorexidina/farmacologia , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Antibacterianos/administração & dosagem , Anti-Infecciosos Locais/administração & dosagem , Anti-Infecciosos Locais/farmacologia , Clorexidina/administração & dosagem , Composição de Medicamentos/métodos , Géis , Poloxâmero/química , Temperatura , Temperatura de Transição , Cicatrização/efeitos dos fármacos
7.
Gels ; 10(3)2024 Feb 21.
Artigo em Inglês | MEDLINE | ID: mdl-38534579

RESUMO

In situ poloxamer-based gels are increasingly being explored as ocular drug delivery carriers to extend the release of active substances, thereby enhancing bioavailability. The objective of this study was to develop thermally stable in situ gels incorporating balsam poplar bud extract, propolis extract, and p-coumaric acid solution and to evaluate the physicochemical parameters of these gelified eye drops. This research assessed the compatibility of poloxamer-based eye drops with active components, their physicochemical properties, stability post-sterilization and during storage, and the release profiles of the active compounds. Fifteen eye drop formulations were prepared and categorized into three groups based on active components. One of the active components was propolis extract. As an alternative to propolis, eye drops containing the plant precursor, balsam poplar bud extract, were developed. The third group's active component was p-coumaric acid, a dominant phenolic acid in propolis and balsam poplar bud extracts. The study reported phenolic contents of 76.63 CAE mg/g for propolis and 83.25 CAE mg/g for balsam poplar bud aqueous extracts, with balsam poplar bud extracts showing higher SPF values (14.0) compared to propolis (12.7), while p-coumaric acid solution exhibited the highest SPF values (25.5). All eye drops were transparent, with pH values meeting the requirements for ocular drops. Formulations containing 8-10% poloxamer 407 met the criteria for in situ gels. All formulations remained stable for 90 days. Conclusion: The study results indicate that the formulated gels possess suitable physicochemical properties, are resistant to applied autoclaving conditions, and exhibit an extended release of active compounds with an increase in poloxamer content.

8.
Vet Sci ; 11(4)2024 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-38668428

RESUMO

Infectious skin diseases are quite common in veterinary medicine. These diseases can be caused by both bacteria and pathogenic fungi. Antimicrobial drugs are usually used for treatment. An alternative to these drugs could be ozonated oils with antibacterial and antifungal properties. Four different ozonated oils (linseed, hemp seed, sunflower, and olive) were tested in order to develop an optimal pharmaceutical form for the treatment of skin infections in animals. Chemical parameters such as acid and acidity value, iodine and peroxide value, viscosity, and infrared spectres were analysed. The ozonation of oils resulted in changes in their chemical composition. The antimicrobial activity of the tested oils was evaluated by determining the minimum inhibitory concentrations and zones of inhibition in agar. After ozonation, the acid content increased in all the tested oils. The highest acidity was found in linseed oil (13.00 ± 0.11 mg KOH/g; 6.1%). Hemp oil, whose acidity was also significant (second only to linseed oil), was the least acidified by ozonation (11.45 ± 0.09 mg KOH/g; 5.75%). After ozonation, the iodine value in oils was significantly reduced (45-93%), and the highest amounts of iodine value remained in linseed (47.50 ± 11.94 g Iodine/100 g oil) and hemp (44.77 ± 1.41 Iodine/100 g oil) oils. The highest number of peroxides after the ozonation of oils was found in sunflower oil (382 ± 9.8 meqO2/kg). It was found that ozonated hemp and linseed oils do not solidify and remain in liquid form when the temperature drops. The results showed a tendency for the reference strains of S. aureus, E. faecalis, and E. coli to have broader zones of inhibition (p < 0.001) than clinical strains. Overall, ozonated linseed oil had the highest antibacterial activity, and ozonated olive oil had the lowest, as determined by both methods. It was found that ozonated linseed oil was the most effective on bacteria, while the most sensitive were S. aureus ATCC 25923, MRSA, and S. pseudointermedius (MIC 13.5 mg/mL, 4.6 mg/mL, and 13.5 mg/mL, respectively, and sterile zones 20.67 ± 0.98 mm, 20.25 ± 0.45 mm, and 18.25 ± 0.45 mm, respectively). The aim and new aspect of this work is the characterisation of selected ozonated vegetable oils, especially hemp oil, according to chemical and antibacterial parameters, in order to select suitable candidates for preclinical and clinical animal studies in the treatment of bacterial or fungal skin infections in terms of safety and efficacy.

9.
Plants (Basel) ; 12(6)2023 Mar 21.
Artigo em Inglês | MEDLINE | ID: mdl-36987086

RESUMO

Cranberry fruits are an important source of anthocyanins and anthocyanidins. The aim of the present study was to investigate the effect of excipients on the solubility of cranberry anthocyanins and their dissolution kinetics as well as on the disintegration time of the capsules. Selected excipients (sodium carboxymethyl cellulose, beta-cyclodextrin and chitosan) were found to affect the solubility and release kinetics of anthocyanins in freeze-dried cranberry powder. Capsule formulations N1-N9 had a disintegration time of less than 10 min, and capsule formulation N10 containing 0.200 g of freeze-dried cranberry powder, 0.100 g of Prosolv (combination of microcrystalline cellulose and colloidal silicon dioxide), and 0.100 g of chitosan had a capsule disintegration time of over 30 min. The total amount of anthocyanins released into the acceptor medium ranged from 1.26 ± 0.06 mg to 1.56 ± 0.03 mg. Capsule dissolution test data showed that the time to release into the acceptor medium was statistically significantly longer for the chitosan-containing capsule formulations compared to the control capsules (p < 0.05). Freeze-dried cranberry fruit powder is a potential source of anthocyanin-rich dietary supplements, and the choice of excipient chitosan could be a suitable solution in capsule formulations providing greater anthocyanin stability and modified release in the gastrointestinal tract.

10.
Gels ; 9(10)2023 Oct 03.
Artigo em Inglês | MEDLINE | ID: mdl-37888369

RESUMO

The bioactive compounds found in cranberry fruit are natural antioxidants, and their consumption reduces the risk of diabetes, cardiovascular disease, cancers, and urinary tract infections. Oral gels with cranberry fruit extract are a promising product that can ensure accurate dosage and release of the active compounds and are suitable for people with dysphagia. The aim of this study was to determine the effect of polymeric materials on the dissolution kinetics of cranberry fruit anthocyanins from gel formulations. Gel formulations were prepared using freeze-dried cranberry fruit extract with different gelling excipients: chitosan (G1-G3), sodium carboxymethylcellulose (G4-G6), and sodium carboxymethylcellulose combined with carbomers (G7-G9). The dissolution test showed that the release of anthocyanins from gel formulations G1-G6 and G9 was most intense within the first 10 min, with little change in the anthocyanin content of the acceptor medium afterwards. For the formulations based on carboxymethyl cellulose and carbomers G7 and G8, the amount of anthocyanins released into the acceptor medium gradually increased, which prolonged the release time of the active compounds. The test for the release of anthocyanins from the semi-solid systems through a hydrophilic membrane revealed that within the first hour, the total amount of anthocyanins released from the modeled gel formulations (G1-G9) was within the range of 6.02%-13.50%. The 1% chitosan (G1) gel formulation released the fastest and highest amount of anthocyanins (70% within 6 h). The other formulations showed a slower release of anthocyanins, and after 6 h, the amount of anthocyanins released from formulations G2-G9 was <57%.

11.
Gels ; 9(10)2023 Oct 17.
Artigo em Inglês | MEDLINE | ID: mdl-37888394

RESUMO

Balsam poplar buds have been used for wound healing and treating irritated skin in traditional medicine. Balsam poplar buds extracts exhibit anti-inflammatory, antioxidant, and antimicrobial effects. In recent years, scientific research has begun to validate some of these traditional uses, leading to an increased interest in balsam poplar buds as a potential source of natural remedies in modern medicine. The study aims to simulate semi-solid pharmaceutical forms with balsam poplar buds extract and evaluate their quality through biopharmaceutical research. The active compounds identified in Lithuanian poplar buds were p-coumaric acid, cinnamic acid, caffeic acid, galangin, pinocembrin, pinobanksin, and salicin. In gels, pH values ranged from 5.85 ± 0.05 to 5.95 ± 0.07. The determined pH values of emulgels ranged from 5.13 ± 0.05 to 5.66 ± 0.15. After 6 h, the release of active compounds from gels and emulgels ranged from 47.40 ± 2.41% to 71.17 ± 3.54. p-coumaric acid dominates in the balsam poplar buds extracts. The pH values of the prepared sem-solid pharmaceutical forms are suitable for use on the skin. The viscosity of the formulations depends on the amount of gelling agent. All formulations showed antioxidant activity. It is relevant to conduct a more extensive study on the influence of the chosen carrier on the release of active compounds from semi-solid formulations with an extract of balsam poplar buds.

12.
Foods ; 12(10)2023 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-37238812

RESUMO

Caffeic acid is a widely distributed phenolic acid. It is described in the scientific literature that caffeic acid has poor solubility. The aim of this study was to improve the solubility of caffeic acid for better dissolution kinetics when administered orally. During the study, oral capsules of different compositions were modeled. The results of the disintegration test revealed that the excipients affected the disintegration time of the capsules. The excipient hypromellose prolonged the disintegration time and dissolution time of caffeic acid. The dissolution kinetics of caffeic acid from capsules depend on the chosen excipients. P407 was more effective compared to other excipients and positively affected the dissolution kinetics of caffeic acid compared to other excipients. When the capsule contained 25 mg of ß-cyclodextrin, 85% of the caffeic acid was released after 60 min. When the capsule contained 25-50 mg poloxamer 407, more than 85.0% of the caffeic acid was released from capsules after 30 min. The research results showed that in order to improve the dissolution kinetics of caffeic acid, one of the important steps is to improve its solubility.

13.
Plants (Basel) ; 11(15)2022 Jul 22.
Artigo em Inglês | MEDLINE | ID: mdl-35893606

RESUMO

Phenolic compounds with miscellaneous biological activities are an interesting component in dermatology and cosmetology practices. The aim of our study was to determine the phenolic compounds released from emulsion, emulgel, gel, ointment, and oleogel formulations penetration into human skin layers, both the epidermis and dermis, and estimate their antioxidant activity. The ex vivo penetration study was performed using Bronaugh type flow-through diffusion cells. Penetration studies revealed that, within 24 h, the chlorogenic acid released from the oleogel penetrated into skin layers to a depth of 2.0 ± 0.1 µg/mL in the epidermis and 1.5 ± 0.07 µg/mL in the dermis. The oleogel-released complex of phenolic compounds penetrating into epidermis showed the strongest DPPH free radical scavenging activity (281.8 ± 14.1 µM TE/L). The study estimated a strong positive correlation (r = 0.729) between the amount of quercetin penetrated into epidermis and the antioxidant activity detected in the epidermis extract. Plant based phenolic compounds demonstrated antioxidant activity and showed great permeability properties through the skin.

14.
Antioxidants (Basel) ; 11(2)2022 Feb 12.
Artigo em Inglês | MEDLINE | ID: mdl-35204255

RESUMO

Phenolic compounds that estimate apple extracts with multifaceted biological effects are potentially valuable for protection against skin disorders. The purpose of our research was to formulate gels and emulgels containing a complex of phenolic compounds of apple extracts and to perform a biopharmaceutical evaluation of semi-solid pharmaceutical forms, determining their antioxidant activity in vitro. HPLC analyses of phenolic compounds were performed. The total amount of phenolic compounds found in the sample of apples from the 'Paprastasis antaninis' cultivar was 1455.5 ± 72.8 µg/g. The release of phenolics from gels and emulgels was assessed by Franz-type diffusion cells. The in vitro release test revealed that phenolic compounds were released from the gel (G1-G6) formulations (70.6-73.8%) compared to the amounts (77.2-83.9%) released from the emulgel (E1-E6) formulations. The largest amount (83.9%) of phenolic compounds was released from the E5 formulation, while the smallest amounts (70.6%) were released from the formulations G3 and G5. The antioxidant activity evaluated by the DPPH and FRAP methods observed in all gel (G1-G6) and emulgel (E1-E6) formulations after 6 h were the strongest, compared to the activities observed in the formulations after 2 or 4 h. Gels and emulgels, which are rich in apple extracts, have strong antioxidant properties and may be promising choices for the development of new, innovative pharmaceutical forms or cosmetics.

16.
Plants (Basel) ; 11(24)2022 Dec 16.
Artigo em Inglês | MEDLINE | ID: mdl-36559670

RESUMO

The growing interest in polyphenols of natural origin and their plant sources encourages the study of their chemical composition and biological activity. Propolis is widely used as a source of phenolic compounds. The aim of this study is to evaluate and compare the chemical composition, antioxidant activity and sun protection factor (SPF) of the ethanolic extracts of the poplar buds, birch buds and pine buds of propolis plant precursors collected in Lithuania. The IC50 concentration of the extracts was evaluated using DPPH and ABTS methods. Extracts of poplar buds, birch buds and propolis showed a lower IC50 concentration by ABTS and DPPH methods compared with pine buds extracts. Poplar buds and propolis extracts showed the highest SPF value, while birch and pine buds extracts showed a lower SPF value. High-performance liquid chromatography (HPLC) analysis results showed that phenolic acids, such as p-coumaric acid and cinnamic acid, and flavonoids, such as pinobanksin and pinocembrin, were identified in all the tested extracts. Salicin has been identified only in poplar buds extracts. The results of antioxidant activity showed that propolis poplar and birch buds are a promising source of biologically active polyphenols.

17.
Antioxidants (Basel) ; 11(9)2022 Sep 08.
Artigo em Inglês | MEDLINE | ID: mdl-36139845

RESUMO

Phenolic compounds of natural origin have been valued for their beneficial effects on health since ancient times. During our study, we performed the extraction of phenolic compounds from balsam poplar buds using different concentrations of aqueous polyethylene glycol 400 solvents (10-30% PEG400). The aqueous 30% PEG400 extract showed the best phenolic yield. The stability of the extract during autoclave sterilization was evaluated. The extract remained stable under heat sterilization. Ophthalmic formulations are formed using different concentrations (8-15%) of poloxamer 407 (P407) together with hydroxypropyl methylcellulose (0.3%), sodium carboxymethyl cellulose (0.3%) or hyaluronic acid (0.1%). Physicochemical parameters of the formulations remained significantly unchanged after sterilization. Formulations based on 12% P407 exhibited properties characteristic of in situ gels, the gelation point of the formulations was close to the temperature of the cornea. After evaluating the amount of released compounds, it was found that, as the concentration of polymers increases, the amount of released compounds decreases. Formulations based on 15% P407 released the least biologically active compounds. Sterilized formulations remained stable for 30 days.

18.
Pharmaceutics ; 14(12)2022 Dec 16.
Artigo em Inglês | MEDLINE | ID: mdl-36559324

RESUMO

Elderflower preparations have long been used to treat colds and flu, but their use is undeservedly reduced, and only dried flower teas, less often ethanolic extracts, can be purchased in pharmacies. In the case of homemade teas, the medicinal plant material is extracted with hot water for a relatively short time, thus only a small part of the active substances is extracted. The industrially produced ethanolic extract is rich in active substances, but its use is limited since ethanol in many countries is undesirable and unsuitable for children and geriatric patients. Therefore, the aim of this work was to produce extracts from elder flowers using water as extractant and a mixture of water + polyethylene glycol (PEG) 20%, to compare their chemical composition and stability, and to study the ability to neutralize reactive oxygen species (ROS) and to sustain the viability of C6 glial cells under oxidative stress conditions. The ethanolic extract was used as a standard. Thus, the extract with PEG contained more than two times higher amount of total phenolics (PC) than the aqueous one, and the stability at 6-8 °C was comparable to the stability of ethanolic extract. All three extracts showed an antioxidant effect in a concentration-dependent manner in vitro. However, only the PEG containing extract (at 20-40 µg/mL PC) was the most effective in reducing the intracellular level of ROS and sustaining the viability of glial cells. The results suggest that the co-solvent PEG increases the yield of phenolics in the extract, prolongs the stability, and enhances positive biological effects.

19.
Medicina (Kaunas) ; 47(6): 354-9, 2011.
Artigo em Lt | MEDLINE | ID: mdl-21968889

RESUMO

BACKGROUND AND OBJECTIVE: Carrier development is one of the essential stages in the formulation of semisolid pharmaceutical dosage form for topical application. The stability of semisolid preparation during storage can be predicted from rheological testing. An adequate composition of semisolid preparation determines its stability and proper release of drug substance, and allows bypassing long-term heating and melting of the cream base components while incorporating complex extracts. Soft propolis extract, well known for its antimicrobial, antiviral, anti-inflammatory, and antioxidant effects, was chosen as a complex biologically active ingredient for the development of emulsion dispersion system. The aim of this study was to evaluate the impact of physical-chemical characteristics of the carrier on the release rate of biologically active ingredients from the modeled dosage form in vitro, thus justifying the relevance of the carrier composition and applied technologies. MATERIAL AND METHODS: Soft propolis extract (1%-3%) was incorporated into water-in-oil type emulsion. The quality of the model systems was evaluated referring to their viscosity, quantity of polyphenols and their rate of release from the preparation by applying an in vitro model. Quantitative determination of polyphenols was performed by spectrophotometry using a standard calibration curve of ferulic acid. RESULTS: The results showed that a stable homogeneous semisolid emulsion system containing soft propolis extract could be produced when the concentration of emulsifier was in the range of 3%-12%. The quantity of emulsifier had an impact on the viscosity of semisolid systems, but practically had no effect on the release rate of polyphenols from the cream matrix. The results also demonstrated that the added amount of soft propolis extract had a less significant effect than temperature of the system. CONCLUSION: It was confirmed that changes in the viscosity of emulsion dispersion systems had no effect on the stability of model dispersion systems when temperature was increased, and this has to be evaluated to determine the storage conditions of the model preparations.


Assuntos
Anti-Infecciosos/química , Preparações de Ação Retardada/química , Portadores de Fármacos/química , Própole/química , Estabilidade de Medicamentos , Emulsões , Viscosidade
20.
Pharmaceuticals (Basel) ; 14(10)2021 Oct 02.
Artigo em Inglês | MEDLINE | ID: mdl-34681242

RESUMO

The balsam poplar (Populus balsamifera L.) buds that grow in Lithuania are a polyphenol-rich plant material with a chemical composition close to that of propolis. In order to potentially adapt the extracts of this plant's raw material for therapeutic purposes, it is important to carry out detailed studies on the chemical composition and biological activity of balsam poplar buds. An important step is to evaluate the yield of polyphenols by different extraction methods and using different solvents. According to our research, extracts of balsam poplar buds collected in Lithuania are dominated by p-coumaric (496.9-13,291.2 µg/g), cinnamic acid (32.9-11,788.5 µg/g), pinobanksin (34.9-1775.5 µg/g) and salicin (215.3-1190.7 µg/g). The antioxidant activity of poplar buds was evaluated by the ABTS (2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid), DPPH (2,2-diphenyl-1-picrylhydrazyl) and FRAP (ferric-reducing antioxidant power) methods, all extracts showed antioxidant activity and the obtained results correlated with the obtained amounts of total phenolic compounds in the extracts (ABTS r = 0.974; DPPH r = 0.986; FRAP r = 0.955, p < 0.01). Studies of antimicrobial activity have shown that ethanolic extracts have an antimicrobal activity effect against Staphylococcus aureus, Enterococcus faecalis and Escherichia coli. The extracts showed a better antimicrobal activity against gram-positive bacteria.

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