Affiliation:
1. Amity Institute of Pharmacy, Amity University, Uttar Pradesh, Sector 125, Noida, 201313, India
2. Hygia
Institute of Pharmaceutical Education and Research, Lucknow, India
3. Central Instrumentation Facility, Birla Institute
of Technology, Mesra, Ranchi, India
Abstract
Background:
Crisaborole (CB), a boron-based compound, is the first topical PDE4 inhibitor
to be approved by the US Food and Drug Administration (2016) for the treatment of Atopic
Dermatitis. It is marketed as a 2% ointment (Eucrisa, Pfizer). However, CB is insoluble in water;
therfore, CB glycersomes were formulated to enhance its permeation flux across the skin.
Objective:
We developed a glycerosomal gel of CB and compared its in vitro release and permeation
flux with the 2% conventional ointment
Methods:
Glycerosomes were prepared using thin film hydration method employing CB, soya
phosphatidylcholine, and cholesterol. The formed film was further hydrated employing a mixture of
phosphate buffer pH 7.4 /glycerin solution containing varying percentages (20,30, 40, and 50 %) of
glycerol. The glycerosomes obtained were characterized by their size, polydispersity index (PDI),
and Zeta potential. The entrapment efficiency of the optimized formulation (F 1) was determined.
The in vitro release of F1 was compared with its 2% conventional ointment. F1 was further incorporated
into carbopol 934 P gel. The gel was characterized by pH, viscosity, spreadability, and drug
content. The permeability flux of the glycerosomal gel was compared with its 2% conventional
ointment.
Results:
The optimized CB glycerosomes had a vesicle size of 137.5 ± 50.58 nm, PDI 0.342, and
zeta potential -65.4 ± 6.75 mV. CB glycerosomal gel demonstrated a 2.13-fold enhancement in the
permeation flux.
Conclusion:
It can thereby be concluded that glycerosomes can be an effective delivery system to
enhance the penetration of CB across the skin.
Publisher
Bentham Science Publishers Ltd.
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