PMID- 34915145
OWN - NLM
STAT- MEDLINE
DCOM- 20220104
LR  - 20220104
IS  - 1873-3476 (Electronic)
IS  - 0378-5173 (Linking)
VI  - 612
DP  - 2022 Jan 25
TI  - Sustainable and efficient skin absorption behaviour of transdermal drug: The 
      effect of the release kinetics of permeation enhancer.
PG  - 121377
LID - S0378-5173(21)01183-2 [pii]
LID - 10.1016/j.ijpharm.2021.121377 [doi]
AB  - At present, how the release kinetics of permeation enhancers affected their 
      enhancement efficacy on drug skin absorption and its molecular mechanisms 
      remained unclear. Herein, the release kinetics of permeation enhancer (Plurol 
      Oleique CC (POCC)) which involved release percent (PR), release duration (RD) and 
      release kinetic constant (k) and its enhancement efficacy on drug skin absorption 
      were investigated with in vitro skin retention study and in vitro skin permeation 
      study, respectively. POCC released from the acidic-drug loading patches followed 
      with the Higuchi release model and had short RD (8-16 h), resulting in its 
      unsustainable enhancement efficiency for acidic drugs. However, POCC released 
      from the basic-drug loading patches followed with zero-order model with long RD 
      (12-24 h), inducing a sustainable and efficient enhancement efficiency for basic 
      drugs. The lower variance of an innovative parameter permeation enhancement 
      coefficient (C(PE)) represented the relatively sustainable and effective 
      enhancement effect and was listed as followed: 0.20 (Zaltoprofen (ZPF)), 0.31 
      (Diclofenac (DCF)), 0.27 (Indomethacin (IMC)), 0.07 (Azasetron (AST)), 0.11 
      (Oxybutynin (OBN)) and 0.06 (Donepezil (DNP)). According to the results of FT-IR, 
      MTDSC, (13)C NMR spectra, molecular dynamics simulation, SAXS and Raman imaging, 
      the Higuchi release model was caused by strong interaction between the acid drugs 
      and pressure sensitive adhesive (PSA). This strong interaction induced faster 
      diffusion speed of POCC from acidic-drug loading patches and make the swell 
      degree of long periodicity phase (LPP) of stratum corneum (SC) lipids reached 
      plateau early. The zero-order release model was because the weak interaction 
      between basic drugs and PSA making most of POCC was still bound to PSA, which in 
      turn lead to LPP swelled at a slow but sustainable process. In conclusion, 
      zero-order release kinetic of POCC lead to sustainable and efficient penetration 
      enhancement efficiency on basic drug, while the Higuchi release kinetic showed 
      opposite effect for acidic drugs. A deep understanding of release kinetics of 
      enhancer and its enhancement efficiency may drive the ideal selection of 
      permeation enhancers and rational optimization of transdermal patches.
CI  - Copyright (c) 2021. Published by Elsevier B.V.
FAU - Ruan, Jiuheng
AU  - Ruan J
AD  - Department of Pharmaceutical Sciences, Shenyang Pharmaceutical University, 103 
      Wenhua Road, Shenyang, Liaoning 110016, China.
FAU - Liu, Chao
AU  - Liu C
AD  - Department of Pharmaceutical Sciences, Shenyang Pharmaceutical University, 103 
      Wenhua Road, Shenyang, Liaoning 110016, China.
FAU - Song, Haoyuan
AU  - Song H
AD  - Department of Pharmaceutical Sciences, Shenyang Pharmaceutical University, 103 
      Wenhua Road, Shenyang, Liaoning 110016, China.
FAU - Zhong, Ting
AU  - Zhong T
AD  - Department of Pharmaceutical Sciences, Shenyang Pharmaceutical University, 103 
      Wenhua Road, Shenyang, Liaoning 110016, China.
FAU - Quan, Peng
AU  - Quan P
AD  - Department of Pharmaceutical Sciences, Shenyang Pharmaceutical University, 103 
      Wenhua Road, Shenyang, Liaoning 110016, China.
FAU - Fang, Liang
AU  - Fang L
AD  - Department of Pharmaceutical Sciences, Shenyang Pharmaceutical University, 103 
      Wenhua Road, Shenyang, Liaoning 110016, China. Electronic address: 
      fangliang2003@yahoo.com.
LA  - eng
PT  - Journal Article
DEP - 20211214
PL  - Netherlands
TA  - Int J Pharm
JT  - International journal of pharmaceutics
JID - 7804127
RN  - 0 (Pharmaceutical Preparations)
SB  - IM
MH  - Administration, Cutaneous
MH  - Kinetics
MH  - *Pharmaceutical Preparations/metabolism
MH  - Scattering, Small Angle
MH  - Skin/metabolism
MH  - *Skin Absorption
MH  - Spectroscopy, Fourier Transform Infrared
MH  - Transdermal Patch
MH  - X-Ray Diffraction
OTO - NOTNLM
OT  - Higuchi release model
OT  - Permeation enhancement coefficient
OT  - Permeation enhancer
OT  - Release kinetic
OT  - Zero-order release model
EDAT- 2021/12/17 06:00
MHDA- 2022/01/05 06:00
CRDT- 2021/12/16 20:20
PHST- 2021/08/31 00:00 [received]
PHST- 2021/11/26 00:00 [revised]
PHST- 2021/12/09 00:00 [accepted]
PHST- 2021/12/17 06:00 [pubmed]
PHST- 2022/01/05 06:00 [medline]
PHST- 2021/12/16 20:20 [entrez]
AID - S0378-5173(21)01183-2 [pii]
AID - 10.1016/j.ijpharm.2021.121377 [doi]
PST - ppublish
SO  - Int J Pharm. 2022 Jan 25;612:121377. doi: 10.1016/j.ijpharm.2021.121377. Epub 
      2021 Dec 14.