Preparation and evaluation of bicyclol microemulsions for enhanced oral bioavailability

Abstract

Of various cosurfactants tested, transcutol provided the most significantly increased solubility of bicyclol (>20 mg/ml). Bicyclol was rapidly dissolved from the premicroemulsion concentrate (approximately 80% within 10 min). Consistent with the improved in vitro profiles, the oral absorption of bicyclol was significantly increased for the premicroemulsion concentrate, i.e. AUC and C(max) were increased by 7.7- and 7.2-fold, respectively, over control values. These findings demonstrate that the microemulsion may be a useful drug delivery system to improve the oral bioavailability of bicyclol.

Effects of PEGylated lipid nanoparticles on the oral absorption of one BCS II drug: a mechanistic investigation

“…These systems include novel solid formulations such as nanocrystals, 2,3 solid dispersions, 4,5 and cyclodextrin inclusion complexes; 6,7 and liquid nanocarriers such as liposomes, 8 micelles, 9 lipid nanoparticles, 10 and micro/nanoemulsions. 11,12 For solid dosage forms, three main factors, ie, solubility, dissolution rate, and intestinal permeability, govern the rate and extent of oral absorption of BCS II drugs. However, as far as liquid nanocarriers are concerned, the oral bioavailability largely depends on the types of carriers and their in vivo fates post-administration.…”

Nanoemulsion improves the oral bioavailability of baicalin in rats: in vitro and in vivo evaluation

“…Cosurfactant was also an important component for the development of nanoemulsion formulations, because a suitable cosurfactant is used to overcome problems related to the poor solubility and low oral bioavailability of drug. 11 Thus, the solubilities of baicalin in three different cosurfactants were studied (Figure 2). Among the cosurfactants examined, PEG400 showed the highest solubility of baicalin (9.328 ± 0.259 mg/mL), followed by propylene glycol (7.056 ± 0.308 mg/mL); ethanol showed the lowest solubility (1.214 ± 0.115 mg/mL).…”

“…10 Nanoemulsions exhibit unique advantages and properties, such as reduced droplet size with larger surface area, improved drug solubility and dissolution rates, and enhanced drug absorption from the gastrointestinal tract by surfactant-induced mucosal permeability changes. [11][12][13][14][15][16][17][18][19] Nanoemulsion formulations have been widely used to overcome problems related to the poor water solubility and low oral bioavailability of some drugs. [20][21][22][23][24][25][26] Therefore, amongst the various drug delivery systems, nanoemulsions are considered an ideal alternative for the oral administration of drugs with poor water solubility, as they improve absorption and bioavailability.…”