Evaluation of critical formulation parameters in design and differentiation of self-microemulsifying drug delivery systems (SMEDDSs) for oral delivery of aciclovir
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, 301-311Publisher:
- Elsevier Science BV, Amsterdam
Funding / projects:
DOI: 10.1016/j.ijpharm.2015.11.011
ISSN: 0378-5173
PubMed: 26611669
WoS: 000367385600032
Scopus: 2-s2.0-84955362408
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Institution/Community
PharmacyTY - 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 . .