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Semisolid self-microemulsifying drug delivery systems (SMEDDSs): Effects on pharmacokinetics of acyclovir in rats

Authorized Users Only
2018
Authors
Đekić, Ljiljana
Janković, Jovana
Rasković, Aleksandar
Primorac, Marija
Article (Published version)
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Abstract
Semisolid self-microemulsifying drug delivery system (SMEDDS) with optimized drug loading capacity, stability, dispersibility in aqueous media and in vitro drug release profile, was evaluated in vivo regarding effects on pharmacokinetics of acyclovir, an antiviral with low bioavailability (BA) and short half-life (t(1/2)). Additional goal of this study was evaluation of safety of this semisolid SMEDDS consisted of medium chain length triglycerides (oil) (10% w/w), macrogolglycerol hydroxystearate (surfactant) (56.25% w/w), polyglyceryl-3-dioleate (cosurfactant) (6.25% w/w), glycerol (cosolvent) (20% w/w), macrogol 8000 (viscosity modifier) (7.5% w/w), and acyclovir (2.5 mg/ml). The study was performed on fully mature white male Wistar rats. The pharmacokinetics of acyclovir was monitored in three groups (1-3) of animals after administration of drug solution (intravenously (IV)), drug suspension (orally) and semisolid SMEDDS (orally), respectively. The determined pharmacokinetic paramet...ers were: maximum concentration of acyclovir in serum (C-max), time taken to reach C-max (T-max), areas under time-concentration curves (AUC(0-t) and AUC(0-infinity)), terminal elimination rate constant (k(el)), t(1/2), volume of distribution (V-d), mean residence time (MRT), clearance (Cl), zero concentration (C-0), steady state volume of distribution (V-ss), and BA. Additionally, for safety evaluation, animals were treated orally with aqueous solution of acyclovir, drug-free semisolid SMEDDS and acyclovir-loaded semisolid SMEDDS, during 21 days (groups 4-7). Serum samples of sacrificed animals were used for biochemical analysis of enzymatic activity of alanine transaminase (ALT) and aspartate transaminase (AST), urea, creatinine, and uric acid. Acyclovir administered by semisolid SMEDDS reached twice higher C-max (0.92 +/- 0.21 mu g/ml) and has significantly shorter T-max (14 +/- 10.84 min) compared to the suspension of acyclovir (C-max 0.29 +/- 0.09 mu g/ml and T-max 26.00 +/- 5.48 min). BA of the drug was significantly increased by semisolid SMEDDS, while the analysis of biochemical parameters excluded damage on function of liver and kidneys caused by the investigated drug delivery system.

Keywords:
Self-microemulsifying drug delivery systems (SMEDDS) / Semisolid SMEDDS / Acyclovir / Wistar rats / Oral bioavailability / Safety
Source:
European Journal of Pharmaceutical Sciences, 2018, 121, 287-292
Publisher:
  • Elsevier Science BV, Amsterdam
Funding / projects:
  • Advanced technologies for controlled release from solid drug delivery systems (RS-34007)

DOI: 10.1016/j.ejps.2018.06.005

ISSN: 0928-0987

PubMed: 29883728

WoS: 000437223600030

Scopus: 2-s2.0-85048641726
[ Google Scholar ]
16
11
URI
https://farfar.pharmacy.bg.ac.rs/handle/123456789/3242
Collections
  • Radovi istraživača / Researchers’ publications
Institution/Community
Pharmacy
TY  - JOUR
AU  - Đekić, Ljiljana
AU  - Janković, Jovana
AU  - Rasković, Aleksandar
AU  - Primorac, Marija
PY  - 2018
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/3242
AB  - Semisolid self-microemulsifying drug delivery system (SMEDDS) with optimized drug loading capacity, stability, dispersibility in aqueous media and in vitro drug release profile, was evaluated in vivo regarding effects on pharmacokinetics of acyclovir, an antiviral with low bioavailability (BA) and short half-life (t(1/2)). Additional goal of this study was evaluation of safety of this semisolid SMEDDS consisted of medium chain length triglycerides (oil) (10% w/w), macrogolglycerol hydroxystearate (surfactant) (56.25% w/w), polyglyceryl-3-dioleate (cosurfactant) (6.25% w/w), glycerol (cosolvent) (20% w/w), macrogol 8000 (viscosity modifier) (7.5% w/w), and acyclovir (2.5 mg/ml). The study was performed on fully mature white male Wistar rats. The pharmacokinetics of acyclovir was monitored in three groups (1-3) of animals after administration of drug solution (intravenously (IV)), drug suspension (orally) and semisolid SMEDDS (orally), respectively. The determined pharmacokinetic parameters were: maximum concentration of acyclovir in serum (C-max), time taken to reach C-max (T-max), areas under time-concentration curves (AUC(0-t) and AUC(0-infinity)), terminal elimination rate constant (k(el)), t(1/2), volume of distribution (V-d), mean residence time (MRT), clearance (Cl), zero concentration (C-0), steady state volume of distribution (V-ss), and BA. Additionally, for safety evaluation, animals were treated orally with aqueous solution of acyclovir, drug-free semisolid SMEDDS and acyclovir-loaded semisolid SMEDDS, during 21 days (groups 4-7). Serum samples of sacrificed animals were used for biochemical analysis of enzymatic activity of alanine transaminase (ALT) and aspartate transaminase (AST), urea, creatinine, and uric acid. Acyclovir administered by semisolid SMEDDS reached twice higher C-max (0.92 +/- 0.21 mu g/ml) and has significantly shorter T-max (14 +/- 10.84 min) compared to the suspension of acyclovir (C-max 0.29 +/- 0.09 mu g/ml and T-max 26.00 +/- 5.48 min). BA of the drug was significantly increased by semisolid SMEDDS, while the analysis of biochemical parameters excluded damage on function of liver and kidneys caused by the investigated drug delivery system.
PB  - Elsevier Science BV, Amsterdam
T2  - European Journal of Pharmaceutical Sciences
T1  - Semisolid self-microemulsifying drug delivery systems (SMEDDSs): Effects on pharmacokinetics of acyclovir in rats
VL  - 121
SP  - 287
EP  - 292
DO  - 10.1016/j.ejps.2018.06.005
ER  - 
@article{
author = "Đekić, Ljiljana and Janković, Jovana and Rasković, Aleksandar and Primorac, Marija",
year = "2018",
abstract = "Semisolid self-microemulsifying drug delivery system (SMEDDS) with optimized drug loading capacity, stability, dispersibility in aqueous media and in vitro drug release profile, was evaluated in vivo regarding effects on pharmacokinetics of acyclovir, an antiviral with low bioavailability (BA) and short half-life (t(1/2)). Additional goal of this study was evaluation of safety of this semisolid SMEDDS consisted of medium chain length triglycerides (oil) (10% w/w), macrogolglycerol hydroxystearate (surfactant) (56.25% w/w), polyglyceryl-3-dioleate (cosurfactant) (6.25% w/w), glycerol (cosolvent) (20% w/w), macrogol 8000 (viscosity modifier) (7.5% w/w), and acyclovir (2.5 mg/ml). The study was performed on fully mature white male Wistar rats. The pharmacokinetics of acyclovir was monitored in three groups (1-3) of animals after administration of drug solution (intravenously (IV)), drug suspension (orally) and semisolid SMEDDS (orally), respectively. The determined pharmacokinetic parameters were: maximum concentration of acyclovir in serum (C-max), time taken to reach C-max (T-max), areas under time-concentration curves (AUC(0-t) and AUC(0-infinity)), terminal elimination rate constant (k(el)), t(1/2), volume of distribution (V-d), mean residence time (MRT), clearance (Cl), zero concentration (C-0), steady state volume of distribution (V-ss), and BA. Additionally, for safety evaluation, animals were treated orally with aqueous solution of acyclovir, drug-free semisolid SMEDDS and acyclovir-loaded semisolid SMEDDS, during 21 days (groups 4-7). Serum samples of sacrificed animals were used for biochemical analysis of enzymatic activity of alanine transaminase (ALT) and aspartate transaminase (AST), urea, creatinine, and uric acid. Acyclovir administered by semisolid SMEDDS reached twice higher C-max (0.92 +/- 0.21 mu g/ml) and has significantly shorter T-max (14 +/- 10.84 min) compared to the suspension of acyclovir (C-max 0.29 +/- 0.09 mu g/ml and T-max 26.00 +/- 5.48 min). BA of the drug was significantly increased by semisolid SMEDDS, while the analysis of biochemical parameters excluded damage on function of liver and kidneys caused by the investigated drug delivery system.",
publisher = "Elsevier Science BV, Amsterdam",
journal = "European Journal of Pharmaceutical Sciences",
title = "Semisolid self-microemulsifying drug delivery systems (SMEDDSs): Effects on pharmacokinetics of acyclovir in rats",
volume = "121",
pages = "287-292",
doi = "10.1016/j.ejps.2018.06.005"
}
Đekić, L., Janković, J., Rasković, A.,& Primorac, M.. (2018). Semisolid self-microemulsifying drug delivery systems (SMEDDSs): Effects on pharmacokinetics of acyclovir in rats. in European Journal of Pharmaceutical Sciences
Elsevier Science BV, Amsterdam., 121, 287-292.
https://doi.org/10.1016/j.ejps.2018.06.005
Đekić L, Janković J, Rasković A, Primorac M. Semisolid self-microemulsifying drug delivery systems (SMEDDSs): Effects on pharmacokinetics of acyclovir in rats. in European Journal of Pharmaceutical Sciences. 2018;121:287-292.
doi:10.1016/j.ejps.2018.06.005 .
Đekić, Ljiljana, Janković, Jovana, Rasković, Aleksandar, Primorac, Marija, "Semisolid self-microemulsifying drug delivery systems (SMEDDSs): Effects on pharmacokinetics of acyclovir in rats" in European Journal of Pharmaceutical Sciences, 121 (2018):287-292,
https://doi.org/10.1016/j.ejps.2018.06.005 . .

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