Phospholipid-based solid drug formulations for oral bioavailability enhancement: A meta-analysis

Liposomes for Enhanced Bioavailability of Water-Insoluble Drugs: In Vivo Evidence and Recent Approaches

“…The mechanisms of oral delivery of liposomes have not been fully understood yet, despite the significant number of in vitro studies on the dissolution and permeation enhancement [8]. According to a meta-analysis performed in 2015, liposomes clearly improved solubility and permeability, showing a 127.4% and 59.5% increase, respectively [10]. Water-insoluble drugs can be solubilized into sub-micron sized liposomes, subsequently being released at a sustained mode in the GI tract or transferred into mixed micelles formed in the presence of bile salts, as suggested in Figure 6.…”

“…However, liposomal oral delivery resurged with a rapid increase in the number of papers published, as shown in Pubmed search results, mainly due to various advanced modification technologies, even though liposomal oral delivery-related papers account for only 5-6% of the total number of liposomes-related studies (Figure 1). In addition, there was an encouraging meta-analysis report in which phospholipid-based solid formulations were analyzed as being effective for BA enhancement [10]. Although liposomal delivery does not seem to achieve satisfactory improvement of oral BA for peptides and protein drugs yet, it looks more promising for oral delivery of hydrophobic drugs because liposomes can solubilize poorly water-soluble drugs, protect the drug from degradation in the GI tract and enhance permeability through the epithelial cell membrane, consequently increasing oral BA.…”

A Liposomal Formulation for Improving Solubility and Oral Bioavailability of Nifedipine

“…In this study, proliposomes were evaluated as a carrier for nifedipine oral administration [13]. Proliposomes have the advantage of continuously releasing drug and stabilizing its blood concentration, and they may improve bioavailability and drug stability [14]. The purpose of preparing proliposomes is improving bioavailability and elimination half-life of nifedipine, which could avoid the blood pressure fluctuations caused by repeated administration and improve therapeutic effects.…”

“…Absorption of lipophilic drugs in intestinal was limited by their restricted dissolution rate. Absorption increasing of proliposomes could be attributed to enhance contact level of drug and the intestinal membrane [14]. Proliposomes could improve the solubility of nifedipine and increase the contact area between the drug and intestinal epithelial cells to improve absorption efficiency.…”

“…Improved bioavailability of nifedipine proliposomes might be caused by intestinal lymphatic transport pathway. It was a one-way channel from the lymphatic system to the blood [14]. Elgart et al found that nanoparticles were taken up in the proximal small intestine by phagocytosis of chylomicron pathway to enter the lymphatic system, which could avoid first-pass metabolism by liver to improve bioavailability [20].…”