Exploration of in vitro drug release testing methods for saquinavir microenvironmental pH modifying buccal films
Research output: Contribution to journal › Journal article › Research › peer-review
Standard
Exploration of in vitro drug release testing methods for saquinavir microenvironmental pH modifying buccal films. / He, Shaolong; Jacobsen, Jette; Nielsen, Carsten Uhd; Genina, Natalja; Østergaard, Jesper; Mu, Huiling.
In: European Journal of Pharmaceutical Sciences, Vol. 163, 105867, 2021.Research output: Contribution to journal › Journal article › Research › peer-review
Harvard
APA
Vancouver
Author
Bibtex
}
RIS
TY - JOUR
T1 - Exploration of in vitro drug release testing methods for saquinavir microenvironmental pH modifying buccal films
AU - He, Shaolong
AU - Jacobsen, Jette
AU - Nielsen, Carsten Uhd
AU - Genina, Natalja
AU - Østergaard, Jesper
AU - Mu, Huiling
N1 - Funding Information: Shaolong He acknowledges the China Scholarship Council ( 201708510087 ) for financial support and the technical support from Søren Michael Nielsen, Rita Wulff Rasmussen, Jens Graff, Mette Frandsen and Dorthe Ørbæk.
PY - 2021
Y1 - 2021
N2 - Buccal films containing a pH modifying excipient may be able to increase bioavailability of drugs with pH-dependent solubility such as saquinavir. Access to suitable in vitro drug release testing methods may facilitate buccal formulation development. This study aimed to explore two release testing methods for characterising buccal films and to elucidate the relationship between microenvironmental pH (pHM, i.e. the pH around the swelling films) and saquinavir release. The Franz diffusion cell method was applicable to investigate the effect of hydroxypropyl methylcellulose (HPMC) grade on saquinavir release. Films containing HPMC K3 LV had a faster saquinavir release than films containing HPMC K100 LV. A UV/Vis imaging method was developed to visualise saquinavir release and pHM changes during the initial dissolution. Within 5 min, the pHM decreased from 6.8 to around 5.4 for HPMC K100 LV-based films containing 11.1 % or 16.6 % (w/w) malic acid. Subsequently, the pHM increased due to increasing concentrations of saquinavir. An increase in malic acid content led to a faster saquinavir release. The combination of methods may be broadly applicable for excipient screening in development of buccal formulations. The imaging approach holds promise for characterizing other pH modifying formulation principles.
AB - Buccal films containing a pH modifying excipient may be able to increase bioavailability of drugs with pH-dependent solubility such as saquinavir. Access to suitable in vitro drug release testing methods may facilitate buccal formulation development. This study aimed to explore two release testing methods for characterising buccal films and to elucidate the relationship between microenvironmental pH (pHM, i.e. the pH around the swelling films) and saquinavir release. The Franz diffusion cell method was applicable to investigate the effect of hydroxypropyl methylcellulose (HPMC) grade on saquinavir release. Films containing HPMC K3 LV had a faster saquinavir release than films containing HPMC K100 LV. A UV/Vis imaging method was developed to visualise saquinavir release and pHM changes during the initial dissolution. Within 5 min, the pHM decreased from 6.8 to around 5.4 for HPMC K100 LV-based films containing 11.1 % or 16.6 % (w/w) malic acid. Subsequently, the pHM increased due to increasing concentrations of saquinavir. An increase in malic acid content led to a faster saquinavir release. The combination of methods may be broadly applicable for excipient screening in development of buccal formulations. The imaging approach holds promise for characterizing other pH modifying formulation principles.
KW - Drug release testing method
KW - Franz diffusion cell
KW - Microenvironmental pH
KW - Saquinavir buccal film
KW - UV/Vis imaging
U2 - 10.1016/j.ejps.2021.105867
DO - 10.1016/j.ejps.2021.105867
M3 - Journal article
C2 - 33951482
AN - SCOPUS:85105881112
VL - 163
JO - Norvegica Pharmaceutica Acta
JF - Norvegica Pharmaceutica Acta
SN - 0928-0987
M1 - 105867
ER -
ID: 272322421