Hyaluronic acid-functionalized bilosomes for targeted delivery of tripterine to inflamed area with enhancive therapy on arthritis

Abstract

Arthritis treatment has been challenging because of low drug exposure to the articular cavity. This study was intended to develop hyaluronic acid (HA)-functionalized bilosomes for targeted delivery of tripterine (Tri), an antiphlogistic phytomedicine, to the inflamed joint via ligand-receptor interaction. Tri-loaded bilosomes (Tri-BLs) with cationic lipid (DOTAP) were prepared by a thin film hydration method followed by HA coating to form HA@Tri-BLs. HA@Tri-BLs were then characterized by particle size (PS), entrapment efficiency (EE), and structural morphology. The in vitro drug release, hemocompatibility test and cellular uptake were performed to examine the formulation performances of HA@Tri-BLs. The in vivo pharmacokinetics and antiarthritic efficacy were evaluated in arthritic models, respectively. The obtained HA@Tri-BLs possessed a PS of 118.5 nm around with an EE of 99.56%. HA@Tri-BLs exhibited excellent cellular uptake and targeted delivery efficiency for Tri, which resulted in elongation of circulatory residence time and enhancement of intra-arthritic bioavailability (799.9% relative to Tri solution). The in vivo antiarthritic efficacy of HA@Tri-BLs was also significantly superior to uncoated Tri-BLs that gave rise to obvious inflammation resolution. Our findings suggest that HA-functionalized bilosomes are a promising vehicle for articular delivery of antiphlogistic drugs to potentiate their efficacy.

Bioactive Apigenin loaded oral nano bilosomes: Formulation optimization to preclinical assessment

“…As the bile salt concentration increases the vesicle size decreases due to reduced surface tension as well as flexibility of BIL. But at high concentration it tends to form aggregates itself ( Yang et al, 2019a , Yang et al, 2019b ). The computer-generated polynomial equation of quadratic model for vesicle size is given bellow (Eq.…”

“…Bilosomes (BIL) is an elastic nano-size vesicle consists of lipid, surfactant and bile salt ( Parashar et al, 2019 ). It is structurally similar to liposome ( Yang et al, 2019a , Yang et al, 2019b ), and protect the drug molecule from the enzymatic degradation into GIT ( Wilkhu et al, 2013 ). The bile salt present in intestine (GIT) limits the capabilities of the conventional vesicle by causing lysis of vesicle membrane and led to early release of entrapped drug or molecule before reaching to the site of action ( Naguib et al, 2020 ).…”

Hyaluronic Acid: A Key Ingredient in the Therapy of Inflammation

“…In vitro, HA@Tri-BLs showed a longer circulation time and an increase in the intra-arthritic bioavailability of Tri, compared to Tri-BLs. HA@Tri-BLs was also shown to have significantly higher antiarthritic efficacy than Tri-BLs, resulting in reduced inflammation in vivo after intravenous injection in rats receiving an injection of complete Freund's adjuvant (CFA) [112].…”

Precise engineering of nanoassembled Corilagin small molecule into supramolecular nanoparticles for the treatment and care against cervical carcinoma

“…In recent times, injectable nanomedicines using Corilagin have been documented by Cattel and study groups, and their analogues display superior water solubility and biocompatibility. The in vitro proliferation ability of small molecules of prodrug identi ed with free Corilagin fragments was not affected by Corilagin amino group acylation [31][32][33][34][35].…”