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Application of miscibility analysis and determination of Soluplus solubility map for development of carvedilol-loaded nanofibers

Само за регистроване кориснике
2017
Аутори
Kaljević, Olivera
Đuriš, Jelena
Čalija, Bojan
Lavrić, Zoran
Kristl, Julijana
Ibrić, Svetlana
Чланак у часопису (Објављена верзија)
Метаподаци
Приказ свих података о документу
Апстракт
Electrospinning was used to produce carvedilol-loaded Soluplus polymer nanofibers using a systematic approach. Miscibility between drug and polymer was determined through calculation of the interaction parameter, chi, and the difference between the total solubility parameters, Delta d(t). A solubility map for Soluplus was obtained by examining different solvent systems, carrying out electrospinning, and characterizing the nanofibers formed. Miscibility studies showed that carvedilol and Soluplus can form a miscible system (chi = -2.3054; Delta delta(t) lt 7.0 MPa1/2). Based on the Soluplus solubility map, acetone: chloroform (90: 10; w/w) represents a suitable solvent system for electrospinning of carvedilol-loaded Soluplus nanofibers. Scanning electron microscopy of these nanofiber samples showed smooth surface morphology. The nanofibers had a regular cylindrical morphology. Beads appeared along the nanofibers more frequently in formulations with lower percentages of carvedilol. Dif...ferential scanning calorimetry showed no melting endothermic peak for carvedilol, which suggests its complete conversion from the crystalline to the amorphous form (at polymer: carvedilol 1: 1). The infrared spectrum of the carvedilol-loaded Soluplus nanofibers showed no characteristic carvedilol peak at 3344.5 cm(-1), which suggests interactions between carvedilol and Soluplus. Dissolution studies of these nanofibers showed improved pure carvedilol dissolution properties, with >85% of the carvedilol released in the first 15 min, versus 20% for pure carvedilol. The use of miscibility analysis and polymer solubility studies demonstrate great technological potential to tackle the challenge for inadequate dissolution of poorly water-soluble drugs.

Кључне речи:
Poorly soluble drugs / Solvent mapping / Electrospinning / Solid dispersions / Solubility enhancement / Interaction parameter
Извор:
International Journal of Pharmaceutics, 2017, 533, 2, 445-454
Издавач:
  • Elsevier Science BV, Amsterdam
Финансирање / пројекти:
  • Развој производа и технологија које обезбеђују жељено ослобађање лековитих супстанци из чврстих фармацеутских облика (RS-34007)
Напомена:
  • Peer-reviewed manuscript: http://147.91.1.136/handle/123456789/3447

DOI: 10.1016/j.ijpharm.2017.05.017

ISSN: 0378-5173

PubMed: 28495583

WoS: 000414188500015

Scopus: 2-s2.0-85019246021
[ Google Scholar ]
14
14
URI
https://farfar.pharmacy.bg.ac.rs/handle/123456789/2882
Колекције
  • Radovi istraživača / Researchers’ publications
Институција/група
Pharmacy
TY  - JOUR
AU  - Kaljević, Olivera
AU  - Đuriš, Jelena
AU  - Čalija, Bojan
AU  - Lavrić, Zoran
AU  - Kristl, Julijana
AU  - Ibrić, Svetlana
PY  - 2017
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/2882
AB  - Electrospinning was used to produce carvedilol-loaded Soluplus polymer nanofibers using a systematic approach. Miscibility between drug and polymer was determined through calculation of the interaction parameter, chi, and the difference between the total solubility parameters, Delta d(t). A solubility map for Soluplus was obtained by examining different solvent systems, carrying out electrospinning, and characterizing the nanofibers formed. Miscibility studies showed that carvedilol and Soluplus can form a miscible system (chi = -2.3054; Delta delta(t)  lt  7.0 MPa1/2). Based on the Soluplus solubility map, acetone: chloroform (90: 10; w/w) represents a suitable solvent system for electrospinning of carvedilol-loaded Soluplus nanofibers. Scanning electron microscopy of these nanofiber samples showed smooth surface morphology. The nanofibers had a regular cylindrical morphology. Beads appeared along the nanofibers more frequently in formulations with lower percentages of carvedilol. Differential scanning calorimetry showed no melting endothermic peak for carvedilol, which suggests its complete conversion from the crystalline to the amorphous form (at polymer: carvedilol 1: 1). The infrared spectrum of the carvedilol-loaded Soluplus nanofibers showed no characteristic carvedilol peak at 3344.5 cm(-1), which suggests interactions between carvedilol and Soluplus. Dissolution studies of these nanofibers showed improved pure carvedilol dissolution properties, with >85% of the carvedilol released in the first 15 min, versus 20% for pure carvedilol. The use of miscibility analysis and polymer solubility studies demonstrate great technological potential to tackle the challenge for inadequate dissolution of poorly water-soluble drugs.
PB  - Elsevier Science BV, Amsterdam
T2  - International Journal of Pharmaceutics
T1  - Application of miscibility analysis and determination of Soluplus solubility map for development of carvedilol-loaded nanofibers
VL  - 533
IS  - 2
SP  - 445
EP  - 454
DO  - 10.1016/j.ijpharm.2017.05.017
ER  - 
@article{
author = "Kaljević, Olivera and Đuriš, Jelena and Čalija, Bojan and Lavrić, Zoran and Kristl, Julijana and Ibrić, Svetlana",
year = "2017",
abstract = "Electrospinning was used to produce carvedilol-loaded Soluplus polymer nanofibers using a systematic approach. Miscibility between drug and polymer was determined through calculation of the interaction parameter, chi, and the difference between the total solubility parameters, Delta d(t). A solubility map for Soluplus was obtained by examining different solvent systems, carrying out electrospinning, and characterizing the nanofibers formed. Miscibility studies showed that carvedilol and Soluplus can form a miscible system (chi = -2.3054; Delta delta(t)  lt  7.0 MPa1/2). Based on the Soluplus solubility map, acetone: chloroform (90: 10; w/w) represents a suitable solvent system for electrospinning of carvedilol-loaded Soluplus nanofibers. Scanning electron microscopy of these nanofiber samples showed smooth surface morphology. The nanofibers had a regular cylindrical morphology. Beads appeared along the nanofibers more frequently in formulations with lower percentages of carvedilol. Differential scanning calorimetry showed no melting endothermic peak for carvedilol, which suggests its complete conversion from the crystalline to the amorphous form (at polymer: carvedilol 1: 1). The infrared spectrum of the carvedilol-loaded Soluplus nanofibers showed no characteristic carvedilol peak at 3344.5 cm(-1), which suggests interactions between carvedilol and Soluplus. Dissolution studies of these nanofibers showed improved pure carvedilol dissolution properties, with >85% of the carvedilol released in the first 15 min, versus 20% for pure carvedilol. The use of miscibility analysis and polymer solubility studies demonstrate great technological potential to tackle the challenge for inadequate dissolution of poorly water-soluble drugs.",
publisher = "Elsevier Science BV, Amsterdam",
journal = "International Journal of Pharmaceutics",
title = "Application of miscibility analysis and determination of Soluplus solubility map for development of carvedilol-loaded nanofibers",
volume = "533",
number = "2",
pages = "445-454",
doi = "10.1016/j.ijpharm.2017.05.017"
}
Kaljević, O., Đuriš, J., Čalija, B., Lavrić, Z., Kristl, J.,& Ibrić, S.. (2017). Application of miscibility analysis and determination of Soluplus solubility map for development of carvedilol-loaded nanofibers. in International Journal of Pharmaceutics
Elsevier Science BV, Amsterdam., 533(2), 445-454.
https://doi.org/10.1016/j.ijpharm.2017.05.017
Kaljević O, Đuriš J, Čalija B, Lavrić Z, Kristl J, Ibrić S. Application of miscibility analysis and determination of Soluplus solubility map for development of carvedilol-loaded nanofibers. in International Journal of Pharmaceutics. 2017;533(2):445-454.
doi:10.1016/j.ijpharm.2017.05.017 .
Kaljević, Olivera, Đuriš, Jelena, Čalija, Bojan, Lavrić, Zoran, Kristl, Julijana, Ibrić, Svetlana, "Application of miscibility analysis and determination of Soluplus solubility map for development of carvedilol-loaded nanofibers" in International Journal of Pharmaceutics, 533, no. 2 (2017):445-454,
https://doi.org/10.1016/j.ijpharm.2017.05.017 . .

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