Nosači/preparati na bazi hijaluronske kiseline za parenteralnu primenu sa posebnim osvrtom na konjugaciju sa taksolom

In recent years, drug delivery systems are especially interesting because they allow therapeutic efficiency and reduce side effects. Conjugates of hyaluronic acid and chemotherapeutic agents, especially taxol, have been recognized as excellent solution for many therapeutic indications. The aim of conjugation of taxol with hyaluronic acid was the toxicity reduction on healthy cells and increase of selectivity on tumor cells. Hyaluronic acid could be used in various pharmaceutical preparations, also in parenteral, because of its biocompatibility and biodegradability. Hyaluronic acid as a carrier belongs to in situ gelling systems, which is passing a phase transition in response to external conditions such as temperature, different pH value or the presence of ions, enabling prolonged effect of the drug substances. Many tumor cells have a large number of receptors for hyaluronic acid, which has a great affinity for the tumor cells. The incorporation of taxol in gelling system of hyaluronic acid provides sustained drug release, increased anticancer activity, reduced damage of healthy cells and increased selectivity on cancer cells.Preparati sa produženim oslobađanjem su poslednjih godina posebno aktuelni jer omogućavaju veću terapijsku efikasnost, smanjuju pojavu neželjenih efekata i omogućavaju ciljano delovanje. Posebno su poslednjih godina interesantni konjugati hijaluronske kiseline i citostatika, a jedan od njih je i taksol, koji pored mnogobrojnih terapijskih indikacija ispoljava i niz neželjenih efekata. Cilj konjugovanja taksola sa hijaluronskom kiselinom je smanjenje toksičnosti na zdravim i povećanje selektivnosti na tumorskim ćelijama. Hijaluronska kiselina se može primenjivati u različitim farmaceutskim preparatima, pa i u parenteralnim, jer ima niz prednosti kao što su biokompatibilnost i biodegradibilnost. Spada u in situ gelirajuće sisteme koji se podvrgavaju faznom prelazu u odgovoru na spoljne stimulanse kao što su temperatura, pH ili prisustvo jona, čime se omogućava produženo dejstvo lekovite supstance. Mnoge tumorske ćelije pokazuju ekspresiju velikog broja receptora za hijaluronsku kiselinu, pa ona ima veliki afinitet za tumorske ćelije. Inkorporiranjem taksola u gelirajući sistem sa hijaluronskom kiselinom omogućava se postepeno oslobađanje leka, povećanje antikancerskog delovanja, smanjuje se oštećenje zdravih ćelija i povećava selektivnost leka

Ispitivanje stabilnosti biljnih preparata

Nowdays, the use of products based on medicinal herbs (phytopreparates) are in scientific focus, both in prevention or in treatment of various diseases. Herbal products have been recognized as an excellent source of bioactive compounds which have positive effects on human health. Beside teas, as standard herbal products, phytopreparations are much more represented as final pharmaceutical form on the market today. Phytopreparations must satisfy standard quality, which means that they must be physically, chemically and microbiological stable and have a high degree of purity. In order to determine the stability, storage conditions, shelf-life of the products, stability tests are conducted, which involving tests of environmental factors influence: temperature, relative humidity, light. Stability tests are performed at different stages of development and production. In accordance with the EMEA (European Agency for Drugs and Medical Devices) for a variety of herbal preparations different specific stability tests are conducted.Danas, sve je veći akcenat na upotrebi preparata na bazi lekovitog bilja (fitopreparata), kako u prevenciji tako i u lečenju različitih oboljenja. Biljni preparati su prepoznati kao odličan izvor bioaktivnih komponenti, koji imaju pozitivne efekte na zdravlje ljudi. Pored čajeva, kao standardnih biljnih proizvoda, danas su na tržištu mnogo više zastupljeni fitopreparati kao finalne farmaceutske forme. Fitopreparati moraju biti standardnog kvaliteta, što podrazumeva da moraju biti fizički, hemijski i mikrobilološki stabilni, da su standardizovanog sastava i da su visokog stepena čistoće. U cilju utvrđivanja koliko je jedan proizvod stabilan, definisanja uslova čuvanja, određivanja roka trajanja, sprovode se ispitivanja stabilnosti, koja podrazumevaju ispitivanja uticaja faktora okoline: temperature, relativne vlažnosti vazduha, svetlosti na promenu kvaliteta gotovog proizvoda. Ispitivanja stabilnosti se izvode u različitim fazama razvoja i proizvodnje. U skladu sa zahtevima EMEA (Evropska agencija za lekove i medicinska sredstva) za različite biljne preparate postavljaju se različiti specifični testovi stabilnosti

Raman spectroscopy associated with chemometrics for determining Origanum oil adulteration

Essential oils (EOs) are complex mixtures of volatile and semivolatile compounds (aldehydes, ketones, alcohols and esters) obtained usually by hydro-distillation from the dry or fresh plant material (seeds, leaves, stems, bark or wood) [1]. Most of the EOs are used in aroma therapy, plant protection (as pesticide), food industry (as food preservatives), perfume industry etc. Because of high demand, EOs are often counterfeited and the quality of EOs is usually controlled by gas chromatography. The aim of this paper is to analyze Origanum oil and its counterfeits by Raman spectroscopy. As an adulterant sunflower oil was used. Adulterated essential oils contained 1, 2, 5, 10, 20, 30, 40, 50, 60, 70, 80, 90 % of sunflower oil. Raman spectra of pure Origano oil and its counterfeits were measured by Witec R300 system equipped with 532 nm laser. Visual inspection of raw spectra led to conclusion that band at 2851 cm-1 is a marker for sunflower oil presence in Origanum oil. However, this band was obvious only when concentration of sunflower oil is higher than, or equal to 10% and could not be seen in lower concentration. In order to reveal presence of this this band in lower concentration, region between 2800 and 3000 cm-1 was subjected to derivatization and then smoothing. Results displayed that Raman spectroscopy in combination with mathematical transformation of spectra can reveal small concentration of unwanted adulterant in Origanum oil

Multiobjective optimization of effect-directed planar chromatography as a promising tool for fast selection of polypotent natural products

Anewmethodforefficiently selecting polypotent natural products is proposed in this study. The method involves using effect-directed HPTLC data and multiobjective optimization algorithms to extract chromatographic signals from HPTLC bioassay images. Three different multiobjective optimization methods, namely Derringer’s desirability approach, Technique for order of preference by similarity to ideal solution (TOPSIS), and Sum of ranking differences (SRD), were applied to the chromatographic signals. In combination with jackknife cross-validation, Derringer’s approach and TOPSIS demonstrated high similarity in finding the best (most polypotent), next to the best, next to the worst, and worst (least polypotent) extracts, while the SRD resulted in slightly different outcomes. Furthermore, a new method for identifying the chromatographic features that characterize the most polypotent extracts was proposed. This method is based on partial least square regression (PLS) and can be used in combination with HPTLC-chemical fingerprints to predict the desirability of new extracts. The resulting PLS models demonstrated high statistical performance with determination coefficients ranging from R 2 = 0.885 in the case of Derringer’s desirability, to 0.986 for TOPSIS. However, the PLS modeling of SRD values was not successful

Chokeberry (Aronia melanocarpa L.) extract loaded in alginate and alginate/inulin system

Chokeberry (Aronia melanocarpa) is a rich source of polyphenols with confirmed health benefits. Microencapsulation tehnique is a promising tool for improving its polyphenols functionality, stability and bioavailability. Electrostatic extrusion process was carried out to obtain microbeads with encapsulated chokeberry extract. The effects of the carrier type (alginate of low and medium viscosity), addition of inulin as filler, and the needle diameter (18, 20, 22 gauges) on the morphological characteristics and release properties of the microbeads were studied. Particles obtained with medium viscosity alginate carrier (1.5% w/v), using inulin as filler (5% w/v) and medium needle size (20 gauges) showed the best results in the release studies. Drying process affected the encapsulation efficiency, the amount of encapsulated polyphenols increased from 0.24 mg GAE/g in hydrogel beads to 3.57 mg GAE/g in freeze dried beads, and the release profile of encapsulated extracts was prolonged to 40 min. SEM micrographs confirmed that the addition of inulin as filler improved the final properties of the microbeads, while FTIR analysis showed that the extract was successfully incorporated into the particles. Due to the extended storage and stability, dry microbeads showed the best potential as a delivery system suitable for pharmaceutical or functional food industry

STABILITY TESTING OF HERBAL MEDICINES

Nowdays, the use of products based on medicinal herbs (phytopreparates) are in scientific focus, both in prevention or in treatment of various diseases. Herbal products have been recognized as an excellent source of bioactive compounds which have positive effects on human health. Beside teas, as standard herbal products, phytopreparations are much more represented as final pharmaceutical form on the market today. Phytopreparations must satisfy standard quality, which means that they must be physically, chemically and microbiological stable and have a high degree of purity. In order to determine the stability, storage conditions, shelf- life of the products, stability tests are conducted, which involving tests of environmental factors influence: temperature, relative humidity, light. Stability tests are performed at different stages of development and production. In accordance with the EMEA (European Agency for Drugs and Medical Devices) for a variety of herbal preparations different specific stability tests are conducted

PHARAMACEUTICAL HYALURONIC ACID BASED CARRIERS FOR PARENTERAL USE, PARTICULARLY CONJUGATES WITH TAXOL: A REVIEW

In recent years, drug delivery systems are especially interesting because they allow therapeutic efficiency and reduce side effects. Conjugates of hyaluronic acid and chemotherapeutic agents, especially taxol, have been recognized as excellent solution for many therapeutic indications. The aim of conjugation of taxol with hyaluronic acid was the toxicity reduction on healthy cells and increase of selectivity on tumor cells. Hyaluronic acid could be used in various pharmaceutical preparations, also in parenteral, because of its biocompatibility and biodegradability. Hyaluronic acid as a carrier belongs to in situ gelling systems, which is passing a phase transition in response to external conditions such as temperature, different pH value or the presence of ions, enabling prolonged effect of the drug substances. Many tumor cells have a large number of receptors for hyaluronic acid, which has a great affinity for the tumor cells. The incorporation of taxol in gelling system of hyaluronic acid provides sustained drug release, increased anticancer activity, reduced damage of healthy cells and increased selectivity on cancer cells