PMID- 29238164
OWN - NLM
STAT- MEDLINE
DCOM- 20180723
LR  - 20220311
IS  - 1177-8881 (Electronic)
IS  - 1177-8881 (Linking)
VI  - 11
DP  - 2017
TI  - A novel transdermal nanoethosomal gel of betahistine dihydrochloride for weight 
      gain control: in-vitro and in-vivo characterization.
PG  - 3377-3388
LID - 10.2147/DDDT.S144652 [doi]
AB  - BACKGROUND: Betahistine dihydrochloride (BDH) is a histamine analog used to 
      control weight gain, with short elimination half-life and gastric irritation as 
      side effects. OBJECTIVE: The aim of the current investigation is to formulate and 
      optimize a topical BDH ethosomal gel for weight gain control. MATERIALS AND 
      METHODS: Box-Behnken design was applied to study the effect of independent 
      variables: phosphatidylcholine (PC), propylene glycol (PG), and ethanol on 
      vesicle size; entrapment efficiency; % drug release; and flux. The morphology and 
      zeta potential of the optimized formulation were evaluated. The % drug release, 
      flux, and pharmacodynamics of the optimized formulation gel were studied. 
      RESULTS: The size and entrapment efficiency percent had a direct positive 
      relationship with the concentration of PC and negative relationship with ethanol 
      and PG. The % drug release and flux decreased with increasing PC and PG, while 
      ethanol enhanced both responses. Regression modeling indicated a good correlation 
      between dependent and independent variables, where F16 was chosen as the 
      optimized formulation. F16 showed well-defined spherical vesicles and zeta 
      potential of -24 mV, and % release from the gel exceeded 99.5% over 16 h with the 
      flux of 0.28 mg/cm(2)/h. Food intake and weight gain of rats were significantly 
      decreased after transdermal application of the BDH ethosomal gel when compared 
      with control, placebo, and BDH gel. The histopathological findings proved the 
      absence of inflammation and decrease in adipose tissue. CONCLUSION: Results 
      obtained showed a significant, sustained transdermal absorption of BDH ethosomal 
      gel and, consequently, a decrease in food intake and weight gain.
FAU - El-Menshawe, Shahira F
AU  - El-Menshawe SF
AD  - Department of Pharmaceutics and Industrial Pharmacy, Beni-Suef University, 
      Beni-Suef.
FAU - Ali, Adel Ahmed
AU  - Ali AA
AD  - Department of Pharmaceutics and Industrial Pharmacy, Beni-Suef University, 
      Beni-Suef.
FAU - Halawa, Abdelkhalk Ali
AU  - Halawa AA
AD  - Department of Pharmaceutics and Clinical Pharmacy, Nahda University, Beni-Suef, 
      Egypt.
FAU - Srag El-Din, Ahmed Sg
AU  - Srag El-Din AS
AD  - Department of Pharmaceutics and Clinical Pharmacy, Nahda University, Beni-Suef, 
      Egypt.
LA  - eng
PT  - Journal Article
DEP - 20171128
PL  - New Zealand
TA  - Drug Des Devel Ther
JT  - Drug design, development and therapy
JID - 101475745
RN  - 0 (Gels)
RN  - X32KK4201D (Betahistine)
SB  - IM
MH  - Adipose Tissue/drug effects
MH  - Administration, Oral
MH  - Animals
MH  - Betahistine/administration & dosage/*pharmacology
MH  - Eating
MH  - Female
MH  - Gels/administration & dosage/pharmacology
MH  - Inflammation/drug therapy
MH  - Nanostructures/administration & dosage/*chemistry
MH  - Particle Size
MH  - Rats
MH  - Surface Properties
MH  - Weight Gain/drug effects
PMC - PMC5713695
OTO - NOTNLM
OT  - Box-Behnken design
OT  - neural histamine
OT  - obesity
OT  - pharmacodynamics
OT  - regression modeling
COIS- Disclosure The authors report no conflicts of interest in this work.
EDAT- 2017/12/15 06:00
MHDA- 2018/07/24 06:00
PMCR- 2017/11/28
CRDT- 2017/12/15 06:00
PHST- 2017/12/15 06:00 [entrez]
PHST- 2017/12/15 06:00 [pubmed]
PHST- 2018/07/24 06:00 [medline]
PHST- 2017/11/28 00:00 [pmc-release]
AID - dddt-11-3377 [pii]
AID - 10.2147/DDDT.S144652 [doi]
PST - epublish
SO  - Drug Des Devel Ther. 2017 Nov 28;11:3377-3388. doi: 10.2147/DDDT.S144652. 
      eCollection 2017.