Abstract
In the present research study, we formulate bilosomes (BMs) of diclofenac (DC) for oral delivery for enhancement of therapeutic efficacy (anti-inflammatory disease). The BMS were prepared by thin film hydration method and optimized by Box–Behnken design (BBD) using cholesterol (A), lipid (B), surfactant (C), and bile salt (D) as formulation factors. Their effects were evaluated on vesicle size (Y1) and entrapment efficacy (Y2). The optimized DC-BMs-opt showed a vesicle size of 270.21 ± 3.76 nm, PDI of 0.265 ± 0.03, and entrapment efficiency of 79.01 ± 2.54%. DSC study result revealed that DC-BMs-opt exhibited complete entrapment of DC in BM matrix. It also depicted significant enhancement (p < 0.05) in release (91.82 ± 4.65%) as compared to pure DC (36.32 ± 4.23%) and DC-liposomes (74.54 ± 4.76%). A higher apparent permeability coefficient (2.08 × 10−3 cm/s) was also achieved compared to pure DC (6.6 × 10−4 cm/s) and DC-liposomes (1.33 × 10−3 cm/s). A 5.21-fold and 1.43-fold enhancement in relative bioavailability was found relative to pure DC and DC liposomes (DC-LP). The anti-inflammatory activity result showed a significant (p < 0.05) reduction of paw edema swelling compared to pure DC and DC-LP. Our findings revealed that encapsulation of DC in BMs matrix is a good alternative for improvement of therapeutic efficacy.
Highlights
IntroductionDiclofenac (DC) is a non-steroidal anti-inflammatory (NSAID) agent with anti-inflammatory and antipyretic activity
diclofenac bilosomes (DC-BMs) were prepared by slightly modified thin-film hydration method [13]
The solution was transferred to a round bottom flask and organic solvent was evaporated at a temperature of 50 ◦ C with reduced pressure using a rotary evaporator (IKA, RV-3V, Staufen, Germany)
Summary
Diclofenac (DC) is a non-steroidal anti-inflammatory (NSAID) agent with anti-inflammatory and antipyretic activity. It is widely used for treatment of acute pain and various antiinflammatory diseases such as osteoarthritis and rheumatoid arthritis. It has a short half-life of 1–2 h due to extensive first-pass metabolism. It belongs to the BCS-II class drug and reported low solubility [1]. The long exposure to DC inhibits prostaglandin formation
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
