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Vrednotenje vpliva učinkovin na lastnosti hidrofilnih nanovlaken
ID Grajzar, Nina (Author), ID Kocbek, Petra (Mentor) More about this mentor... This link opens in a new window, ID Dragar, Črt (Comentor)

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Abstract
Polimerna nanovlakna veljajo za enega bolj obetavnih nanodostavnih sistemov, ki ga odlikujejo edinstvene lastnosti nanomaterialov, kot sta velika specifična površina in poroznost mreže nanovlaken, kar lahko pomembno vpliva na topnost in hitrost raztapljanja v nanovlakna vgrajenih zdravilnih učinkovin. Lastnosti nanovlaken so odvisne predvsem od lastnosti osnovnih gradnikov (tj. polimerov), uporabljenih pomožnih snovi in metode ter pogojev izdelave, nenazadnje pa bi nanje lahko pomembno vplivale tudi lastnosti vgrajene zdravilne učinkovine. Namen magistrske naloge je tako bil proučiti vpliv vgradnje zdravilne učinkovine na lastnosti izdelanih nanovlaken. S procesom elektrostatskega sukanja smo izdelali nanovlakna iz polietilenoksida in poloksamera 188 v masnem razmerju 1:1, v katera smo vgradili 20 % (m/m) ene izmed štirih proučevanih zdravilnih učinkovin. Za vgradnjo smo izbrali zdravilne učinkovine z različnimi fizikalno-kemijskimi lastnostmi, in sicer ibuprofen, karvedilol, paracetamol in metforminijev klorid. Nanovlakna z različnimi zdravilnimi učinkovinami smo izdelali pri enakih pogojih izdelave (odmik zbirala od konice igle 15 cm; električna napetost 15 kV, zunanji premer igle 0,7 mm; pretok polimerne raztopine 1,40 mL/h; čas elektrostatskega sukanja ~2 h; relativna vlažnost < 50 %; sobna temperatura) in jih natančno ovrednotili. Ugotovili smo, da različne fizikalno-kemijske lastnosti zdravilnih učinkovin ne vplivajo pomembno na potek elektrostatskega sukanja in na nastanek nanovlaken. Dokazali smo, da vgradnja zdravilnih učinkovin, ki pomembno vplivajo na viskoznost raztopine za elektrostatsko sukanje, vodi v nastanek prekinjenih nanovlaken, ki se med seboj zlivajo, medtem ko vgradnja zdravilnih učinkovin s slabšo topnostjo v 96 % (V/V) etanolu vodi v nastanek nanovlaken z delci na površini nanovlaken. Ugotovili smo, da zdravilne učinkovine s hidroksilno skupino v strukturi tvorijo vodikove vezi s polimeroma v ogrodju nanovlaken, kar bi utegnilo pomembno vplivati na stabilnost vgrajene amorfne oblike zdravilne učinkovine. Na podlagi dobljenih rezultatov smo ugotovili tudi, da vgradnja bolj hidrofobnih zdravilnih učinkovin zmanjša hidrofilnost površine nanovlaken, medtem ko vgradnja bolj hidrofilnih na lastnosti površine nanovlaken ne vpliva bistveno. Dokazali smo, da je učinkovitost vgradnje zdravilne učinkovine v nanovlakna neodvisna od lastnosti le-te, na profil sproščanja zdravilne učinkovine iz nanovlaken pa pomembno vplivata morfologija nanovlaken in njihova hitrost dispergiranja v mediju za sproščanje. Izsledki našega raziskovalnega dela tako prinašajo nova znanja na področju izdelave polimernih nanovlaken kot dostavnih sistemov.

Language:Slovenian
Keywords:Dostavni sistem, elektrostatsko sukanje, nanovlakna, polietilenoksid, poloksamer 188
Work type:Master's thesis/paper
Organization:FFA - Faculty of Pharmacy
Year:2024
PID:20.500.12556/RUL-158944 This link opens in a new window
Publication date in RUL:23.06.2024
Views:81
Downloads:16
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Secondary language

Language:English
Title:Evaluation of drugs impact on the properties of hydrophilic nanofibers
Abstract:
Polymer nanofibers are a promising nanosystem for drug delivery due to the unique properties of the materials in nanoscale dimensions, such as high specific surface area, and porosity of the nanofiber mat. These properties can significantly improve the solubility and dissolution rate of drugs incorporated in the nanofibers. The nanofiber properties are affected by the matrix-forming polymers, excipients, and the manufacturing method and conditions. The inclusion of drugs may also have a significant impact on nanofiber properties. Thus, this study aimed to examine how the incorporation of drugs affects the properties of the nanofibers. Nanofibers were produced by electrospinning of polyethylene oxide and poloxamer 188 in a 1:1 weight ratio, and by incorporation of 20% (w/w) of one of four drugs with different physicochemical properties, namely ibuprofen, carvedilol, paracetamol, or metformin hydrochloride. Nanofibers were electrospun under identical conditions (needle tip-to-collector distance, 15 cm; voltage, 15 kV; needle outer diameter, 0.7 mm; polymer solution flow rate, 1.40 mL/h; electrospinning time, ~2 h; relative humidity < 50%; room temperature), followed by precise characterization. We showed that different properties of the drugs do not significantly affect the electrospinning process or the formation of nanofibers. However, the incorporation of drugs, which have a considerable impact on the viscosity of the electrospinning solution, resulted in the creation of non-continuous fused nanofibers. Furthermore, the study revealed that the incorporation of drugs with lower solubility in 96% (v/v) ethanol results in nanofibers with particles on the surface of nanofibers. Additionally, it was demonstrated that drugs containing a hydroxyl group in their structure form hydrogen bonds with the polymers in nanofibers, which may significantly affect the stability of the amorphous form of the drug in the nanofibers. It was also shown that more hydrophobic drugs decrease the hydrophilicity of the nanofiber surface, while more hydrophilic drugs do not have a significant effect on the hydrophilicity of the nanofiber surface. According to our results, the drug incorporation efficiency is not dependent on the properties of the drug. However, the release profile of the drug from nanofibers is significantly affected by the morphology of the nanofibers and their dispersibility in the drug-release medium. Our findings have brought new knowledge to research in the field of preparation of polymer nanofibers as delivery systems.

Keywords:Delivery system, electrospinning, nanofibers, polyethylene oxide, poloxamer 188

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