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Transdermal microemulsions of Boswellia carterii Bird (Study (ตัวแปร…
Transdermal microemulsions
of Boswellia carterii Bird
Introduction
Boswellia species
Boswellia carterii (BC)
Boswellia serrata (BS)
Boswellia resin
Boswellic acid (BA)
steroidal (lipophilic)
acetyl-11-keto-beta-boswellic acid (AKBA)
The strongest inhibitory efficacy
11-keto-beta-boswellic acid (KBA)
Selectively inhibit leukotriene synthesis 5-LO
do not solubilize in the intestional fluid
limited systemic bioavailability
side effects
abdominal discomfort
nausea
epigastric pain
hypergasidity
diarrhea
Other substances
Microemulsions (MEs)
Transparent
low viscous
optically isotropic
thermodynamically stable colloidal dispersion of oil and water
Transdermal (TD)
enhance penetration of substances into and through biologic membrane
easy to formulate
low viscocity
self-preservative property
Material and methods
Methods
Extraction of biologically active fraction
Used Soxhlet apparatus
chromatographic technique to investigate phytochemical
Determination of AKBA content
The AKBA content was estimated as 6.45%± 0.46
detected and identified using NMR, ESI/MS, LC/MS
HPLC
Construction
Pseudo-ternary phase diagrams
Oil : Capmul MCM C8
Surfactant: Tween80 and Labrasol
Tween80 reached higher ME zone
Tween 80 has minimal toxicity
Co-surfactant: PEG400
Water
Selected based on solubility study
enlarged region MEs
Ratio of oil decrease
Smix increase
Preparation of MEs
Determine drug content
ME4
Drug encap 100%
Smix Ratio 2:1
Oil 17.5%
ME1
Drug encap 83%
Oil 7.78%
Smix Ratio 1:1
Characterization of optimized MEs
pH measurement
Electrical conduction
TEM
Globule size&PDI
ex vivo permeation study
Abdominal skin of female Wistar rats
using HPLC
AKBA permeated
ME1 97%
ME4 30%
skin irritancy
Erythema scores of both MEs are close to the control
Experiments
Gr2 0.8% formalin (standard irritant)
Gr3 ME1 test group
Gr1 no application (control)
Gr4 ME4 test group
Carrageenan paw edema test
Tests
Gr2 0.5% piroxicam
(standard transdermal anti-inflammatory)
Gr3 ME1 test group
Gr1 no application (control)
Gr4 ME4 test group
ME1 exhibits significantly higher anti-inflammatory effect
compared to both
Materials
Dried oleogum resin of BC bird
Tween80 (Polysorbate80)
AKBA
PEG 400
Carrageenan
Labrasol
Methanol for HPLC
Conclusion
Successful formulation transdermal
microemulsion delivery systems
optimized microemulsions
suitable pH
non-irritant properties
low globule size
ME1 proved to be superior over ME4
Study
ตัวแปร
ตัวแปรต้น
ME formulations
ME1
ME4
ตัวแปรตาม
Skin irritancy
ex vivo permeation
Characterizations
in vivo anti-inflammatory
ตัวแปรควบคุม
Methods
Materials
สถิติที่ใช้
One way ANOVA
ชนิดของงานวิจัย
Medical research
Applied research
Ethical Aspect
All experiments employing
animals approved