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

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2017
Application_of_miscibility_acc_2017.pdf (1.358Mb)
Authors
Kaljević, Olivera
Đuriš, Jelena
Čalija, Bojan
Lavrić, Zoran
Kristl, Julijana
Ibrić, Svetlana
Article (Accepted Version)
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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. 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.

Keywords:
Poorly soluble drugs / Solvent mapping / Electrospinning / Solid dispersions / Solubility enhancement / Interaction parameter
Source:
International Journal of Pharmaceutics, 2017, 533, 2, 445-454
Publisher:
  • Elsevier
Funding / projects:
  • Advanced technologies for controlled release from solid drug delivery systems (RS-34007)
In:
  • This is peer-reviewed version of the following article: 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. International Journal of Pharmaceutics 2017, 533 (2), 445–454. https://doi.org/10.1016/j.ijpharm.2017.05.017

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/123456789/3447
Collections
  • Radovi istraživača / Researchers’ publications
Institution/Community
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/123456789/3447
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
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",
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., 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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