Biodistribution, pharmacodynamics and pharmacokinetics of oral delivery of exendin-4 using pH-sensitive nanoparticles

阮胡玉

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Biodistribution, pharmacodynamics and pharmacokinetics of oral delivery of exendin-4 using pH-sensitive nanoparticles

利用pH敏感奈米微粒載體口服Exendin-4之生物分佈,藥物動力學及藥效學探討

阮胡玉 , Masters　　Advisor：宋信文　　

英文

促胰島素分泌素；甲殼素；聚服胺酸；生物分佈；藥效學；藥物動力學；大鼠胰島素； exendin-4 ； chitosan ； poly-γ-glutamic acid ； biodistribution ； pharmacodnamic ； pharmacokinetic ； rat insulin

Abstract │ Reference (137) │ Altmetrics

Abstract 〈TOP〉

Abstract 
  Exendin-4 is a 39-amino acid peptide that shares several glucoregulatory activities with
the  mammalian  incretin  hormone,  glucagon-like  peptide-1  (GLP-1).  The  synthetic  form  of 
exendin-4, exenatide, was approved as adjunctive therapy by subcutaneous injection for patients 
with type 2 diabetes failing to achieve glycemic control with oral antidiabetic agents. Basically, 
the oral route is the most convenient way of drug administration for patients because it can avoid 
pain  and  reduce  the  complex  complication.  Base  on  our  previous  study,  we  developed 
nanoparticles (NPs) composed of chitosan (CS), poly-γ-glutamic acid (γPGA) with Fe ions as the 
carrier for exendin-4 delivery via the oral route. The size and zeta potential of the prepared NPs 
were ~300nm and ~30mV, respectively. The exendin-4 loaded in NPs could get ~60% loading 
efficiency  (LE)  and  ~15%  Loading  Content  (LC).  To  protect  NPs  in  the  acidic  stomach 
environment,  gelatin  hard  capsules  filled  with  NPs  were  coated  with  enteric  coating  polymer. 
The enteric coating polymer, Eudragit L55-100, was dissolved beyond pH 6.0 that mimetic the 
pH environment of duodenum in the GI track. In the dissolution study, the test capsule could be 
dissolved immediately as it reached the duodenal region and NPs could then release exendin-4 
into  the  systemic  circulation  via  the  opened  paracellular  pathway.  For  the  in  vivo  study,  the 
biodistribution of exendin-4 loaded NPs following the oral administration to rats was performed 
using the single-photon emission computed tomography (SPECT)/computed tomography (CT). 
The results obtained in the SPECT/CT study indicate that the orally administered exendin-4 was 
significantly absorbed into the systemic circulation. There was very high circulating exendin-4 
(~48%) in the peripheral tissue and plasma (PP) at 2 h post ingestion. In the pharmacodynamic 
(PD) and pharmacokinetic (PK) evaluation in a mild diabetic rat model, the orally administered 
exendin-4 loaded NPs produced a slower hypoglycemic response for a prolonged period of time. 
The relative bioavailability of exendin-4 orally delivered by test NPs in gelatin capsules coated 
with 10% Eudragit was found to be 13.7 ± 2.1%. The results suggest the suitability of the NP 
system to be used as a non-invasive alternative for the basal exendin-4 therapy.

Reference ( 137 ) 〈TOP〉

[1] J.H. Hamman, G.M. Enslin, A.F. Kotze, Oral delivery of peptide drugs: barriers and
連結：
developments, Bio Drugs 19 (2005) 165–177.
連結：
Pharm. Res. 13 (1996) 1760–1764.
連結：
[4] Zambanini A, Newson RB, Maisey M, Feher MD. Injection related anxiety in insulin-
連結：
treated diabetes. Diabetes Res Clin Pract 1999;46(3):239–46.
連結：

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