ABSORPTION ENHANCERS IN NASAL DRUG DELIVERY - EFFICACY AND SAFETY

被引:109
作者
MERKUS, FWHM
SCHIPPER, NGM
HERMENS, WAJJ
ROMEIJN, SG
VERHOEF, JC
机构
[1] Center for Bio-Pharmaceutical Sciences, Leiden University, Leiden
关键词
NASAL DRUG DELIVERY; ABSORPTION ENHANCER; INTERSPECIES DIFFERENCE; MORPHOLOGY; CILIARY MOVEMENT; TOXICITY;
D O I
10.1016/0168-3659(93)90179-9
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Efficacy and safety of nasal absorption enhancers depend on many different parameters, such as their influence on nasal epithelial membrane barriers, the enzymatic activities in the nasal cavity, and the mucociliary clearance. Large interspecies differences appear to exist in the nasal absorption of drugs. Nasal absorption enhancers, although very effective in some cases, differ substantially in efficacy and safety. For a number of enhancers like surfactants, bile salts and fusidate derivatives a good relationship (similarity in rank order) can be established between the morphological damage and the influence on the ciliary beat frequency (CBF) of nasal epithelial tissue, making CBF measurements a valuable tool in the search for safe nasal absorption enhancers.
引用
收藏
页码:201 / 208
页数:8
相关论文
共 38 条
[1]   BIOAVAILABILITY OF LEUPROLIDE ACETATE FOLLOWING NASAL AND INHALATION DELIVERY TO RATS AND HEALTHY HUMANS [J].
ADJEI, A ;
SUNDBERG, D ;
MILLER, J ;
CHUN, A .
PHARMACEUTICAL RESEARCH, 1992, 9 (02) :244-249
[2]   THE EFFECT OF SODIUM TAURO-24,25-DIHYDROFUSIDATE ON THE NASAL ABSORPTION OF HUMAN GROWTH-HORMONE IN 3 ANIMAL-MODELS [J].
BALDWIN, PA ;
KLINGBEIL, CK ;
GRIMM, CJ ;
LONGENECKER, JP .
PHARMACEUTICAL RESEARCH, 1990, 7 (05) :547-552
[3]  
BRAGA PC, 1990, ARZNEIMITTEL-FORSCH, V40-2, P938
[4]   NASAL ABSORPTION IN THE RAT .1. A METHOD TO DEMONSTRATE THE HISTOLOGICAL EFFECTS OF NASAL FORMULATIONS [J].
CHANDLER, SG ;
ILLUM, L ;
THOMAS, NW .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1991, 70 (1-2) :19-27
[5]   NASAL ABSORPTION IN RATS .2. EFFECT OF ENHANCERS ON INSULIN ABSORPTION AND NASAL HISTOLOGY [J].
CHANDLER, SG ;
ILLUM, L ;
THOMAS, NW .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1991, 76 (1-2) :61-70
[6]  
Chien Y. W., 1989, NASAL SYSTEMIC DRUG
[7]   ABSORPTION OF RECOMBINANT METHIONYL-HUMAN GROWTH-HORMONE (MET-HGH) FROM RAT NASAL-MUCOSA [J].
DAUGHERTY, AL ;
LIGGITT, HD ;
MCCABE, JG ;
MOORE, JA ;
PATTON, JS .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1988, 45 (03) :197-206
[8]   ABSORPTION ENHANCEMENT OF INTRANASALLY ADMINISTERED INSULIN BY SODIUM TAURODIHYDROFUSIDATE (STDHF) IN RABBITS AND RATS [J].
DEURLOO, MJM ;
HERMENS, WAJJ ;
ROMEYN, SG ;
VERHOEF, JC ;
MERKUS, FWHM .
PHARMACEUTICAL RESEARCH, 1989, 6 (10) :853-856
[9]   BILE-SALTS AND INTRANASAL DRUG ABSORPTION [J].
DUCHATEAU, GSMJE ;
ZUIDEMA, J ;
MERKUS, FWHM .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1986, 31 (03) :193-199
[10]   THE EFFECTS OF PERMEATION ENHANCERS ON THE SURFACE-MORPHOLOGY OF THE RAT NASAL-MUCOSA - A SCANNING ELECTRON-MICROSCOPY STUDY [J].
ENNIS, RD ;
BORDEN, L ;
LEE, WA .
PHARMACEUTICAL RESEARCH, 1990, 7 (05) :468-475