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Evaluation of critical formulation parameters in design and differentiation of self-microemulsifying drug delivery systems (SMEDDSs) for oral delivery of aciclovir

Authorized Users Only
2016
Authors
Janković, Jovana
Đekić, Ljiljana
Dobričić, Vladimir
Primorac, Marija
Article (Published version)
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Abstract
The study investigated the influence of formulation parameters for design of self-microemulsifying drug delivery systems (SMEDDSs) comprising oil (medium chain triglycerides) (10%), surfactant (Labrasol (R), polysorbate 20, or Kolliphor (R) RH40), cosurfactant (Plurol (R) Oleique CC 497) (q.s. ad 100%), and cosolvent (glycerol or macrogol 400) (20% or 30%), and evaluate their potential as carriers for oral delivery of a poorly permeable antivirotic aciclovir (acyclovir). The drug loading capacity of the prepared formulations ranged from 0.18-31.66 mg/ml. Among a total of 60 formulations, three formulations meet the limits for average droplet size (Z-ave) and polydispersity index (PdI) that have been set for SMEDDSs (Z-ave lt = 100 nm, PdI lt 0.250) upon spontaneous dispersion in 0.1 M HCl and phosphate buffer pH 7.2. SMEDDSs with the highest aciclovir loading capacity (24.06 mg/ml and 21.12 mg/ml) provided the in vitro drug release rates of 0.325 mg cm (2) min (1) and 0.323 mg cm (2...) min (1), respectively, and significantly enhanced drug permeability in the parallel artificial membrane permeability assay (PAMPA), in comparison with the pure drug substance. The results revealed that development of SMEDDSs with enhanced drug loading capacity and oral delivery potential, required optimization of hydrophilic ingredients, in terms of size of hydrophilic moiety of the surfactant, surfactant-to-cosurfactant mass ratio (Km), and log P of the cosolvent.

Source:
International Journal of Pharmaceutics, 2016, 497, 1-2, 301-311
Publisher:
  • Elsevier Science BV, Amsterdam
Funding / projects:
  • Advanced technologies for controlled release from solid drug delivery systems (RS-34007)

DOI: 10.1016/j.ijpharm.2015.11.011

ISSN: 0378-5173

PubMed: 26611669

WoS: 000367385600032

Scopus: 2-s2.0-84955362408
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15
URI
https://farfar.pharmacy.bg.ac.rs/handle/123456789/2579
Collections
  • Radovi istraživača / Researchers’ publications
Institution/Community
Pharmacy
TY  - JOUR
AU  - Janković, Jovana
AU  - Đekić, Ljiljana
AU  - Dobričić, Vladimir
AU  - Primorac, Marija
PY  - 2016
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/2579
AB  - The study investigated the influence of formulation parameters for design of self-microemulsifying drug delivery systems (SMEDDSs) comprising oil (medium chain triglycerides) (10%), surfactant (Labrasol (R), polysorbate 20, or Kolliphor (R) RH40), cosurfactant (Plurol (R) Oleique CC 497) (q.s. ad 100%), and cosolvent (glycerol or macrogol 400) (20% or 30%), and evaluate their potential as carriers for oral delivery of a poorly permeable antivirotic aciclovir (acyclovir). The drug loading capacity of the prepared formulations ranged from 0.18-31.66 mg/ml. Among a total of 60 formulations, three formulations meet the limits for average droplet size (Z-ave) and polydispersity index (PdI) that have been set for SMEDDSs (Z-ave  lt = 100 nm, PdI  lt  0.250) upon spontaneous dispersion in 0.1 M HCl and phosphate buffer pH 7.2. SMEDDSs with the highest aciclovir loading capacity (24.06 mg/ml and 21.12 mg/ml) provided the in vitro drug release rates of 0.325 mg cm (2) min (1) and 0.323 mg cm (2) min (1), respectively, and significantly enhanced drug permeability in the parallel artificial membrane permeability assay (PAMPA), in comparison with the pure drug substance. The results revealed that development of SMEDDSs with enhanced drug loading capacity and oral delivery potential, required optimization of hydrophilic ingredients, in terms of size of hydrophilic moiety of the surfactant, surfactant-to-cosurfactant mass ratio (Km), and log P of the cosolvent.
PB  - Elsevier Science BV, Amsterdam
T2  - International Journal of Pharmaceutics
T1  - Evaluation of critical formulation parameters in design and differentiation of self-microemulsifying drug delivery systems (SMEDDSs) for oral delivery of aciclovir
VL  - 497
IS  - 1-2
SP  - 301
EP  - 311
DO  - 10.1016/j.ijpharm.2015.11.011
ER  - 
@article{
author = "Janković, Jovana and Đekić, Ljiljana and Dobričić, Vladimir and Primorac, Marija",
year = "2016",
abstract = "The study investigated the influence of formulation parameters for design of self-microemulsifying drug delivery systems (SMEDDSs) comprising oil (medium chain triglycerides) (10%), surfactant (Labrasol (R), polysorbate 20, or Kolliphor (R) RH40), cosurfactant (Plurol (R) Oleique CC 497) (q.s. ad 100%), and cosolvent (glycerol or macrogol 400) (20% or 30%), and evaluate their potential as carriers for oral delivery of a poorly permeable antivirotic aciclovir (acyclovir). The drug loading capacity of the prepared formulations ranged from 0.18-31.66 mg/ml. Among a total of 60 formulations, three formulations meet the limits for average droplet size (Z-ave) and polydispersity index (PdI) that have been set for SMEDDSs (Z-ave  lt = 100 nm, PdI  lt  0.250) upon spontaneous dispersion in 0.1 M HCl and phosphate buffer pH 7.2. SMEDDSs with the highest aciclovir loading capacity (24.06 mg/ml and 21.12 mg/ml) provided the in vitro drug release rates of 0.325 mg cm (2) min (1) and 0.323 mg cm (2) min (1), respectively, and significantly enhanced drug permeability in the parallel artificial membrane permeability assay (PAMPA), in comparison with the pure drug substance. The results revealed that development of SMEDDSs with enhanced drug loading capacity and oral delivery potential, required optimization of hydrophilic ingredients, in terms of size of hydrophilic moiety of the surfactant, surfactant-to-cosurfactant mass ratio (Km), and log P of the cosolvent.",
publisher = "Elsevier Science BV, Amsterdam",
journal = "International Journal of Pharmaceutics",
title = "Evaluation of critical formulation parameters in design and differentiation of self-microemulsifying drug delivery systems (SMEDDSs) for oral delivery of aciclovir",
volume = "497",
number = "1-2",
pages = "301-311",
doi = "10.1016/j.ijpharm.2015.11.011"
}
Janković, J., Đekić, L., Dobričić, V.,& Primorac, M.. (2016). Evaluation of critical formulation parameters in design and differentiation of self-microemulsifying drug delivery systems (SMEDDSs) for oral delivery of aciclovir. in International Journal of Pharmaceutics
Elsevier Science BV, Amsterdam., 497(1-2), 301-311.
https://doi.org/10.1016/j.ijpharm.2015.11.011
Janković J, Đekić L, Dobričić V, Primorac M. Evaluation of critical formulation parameters in design and differentiation of self-microemulsifying drug delivery systems (SMEDDSs) for oral delivery of aciclovir. in International Journal of Pharmaceutics. 2016;497(1-2):301-311.
doi:10.1016/j.ijpharm.2015.11.011 .
Janković, Jovana, Đekić, Ljiljana, Dobričić, Vladimir, Primorac, Marija, "Evaluation of critical formulation parameters in design and differentiation of self-microemulsifying drug delivery systems (SMEDDSs) for oral delivery of aciclovir" in International Journal of Pharmaceutics, 497, no. 1-2 (2016):301-311,
https://doi.org/10.1016/j.ijpharm.2015.11.011 . .

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