Bilosomes are innovative vesicular carriers containing
bile salt with a non-ionic
surfactant. Being highly flexible, bilosomes can squeeze themselves through the skin carrying the
drug to the action site and improving its skin penetration. The objective of this research was to encapsulate
niflumic acid (NA), a non-steroidal anti-inflammatory
drug into Brij® integrated bilosomes (BIBs) for effective treatment of
osteoarthritis through transdermal delivery. BIBs were formulated using 100 mg of
Span 20 with different amounts of
sodium cholate (NaC),
sodium taurocholate (NaTC), or
sodium glycocholate (NaGC) as
bile salt, with the addition of 5 mg of Brij-93 or
Brij-35. BIBs were prepared utilizing
ethanol injection method with the application of (31 × 22) complete factorial design using Design-Expert® software. The optimal BIBs formulation determined was (B5) which contains 5 mg of NaTC used as
bile salt and 5 mg of Brij-93. B5 exhibited entrapment efficiency% = 95.21 ± 0.00%, particle size = 373.05 ± 0.07 nm, polydispersity index = 0.27 ± 0.01, and zeta potential = -32.00 ± 0.00 mV. It also had a high elasticity with a spherical shape. B5 gel displayed a sustained release profile with a significantly 2.3 folds' higher
drug permeation percent across rat skin than that permeated from NA gel. Moreover, in vivo anti-osteoarthritic and histopathological studies assured the efficacy and safety of B5 gel and its superiority over NA gel. Generally, the outcomes confirmed the great efficacy of NA loaded BIBs for the topical treatment of
osteoarthritis.