ArticlePharmaceutical research2013
In vitro lipolysis and intestinal transport of β-arteether-loaded lipid-based drug delivery systems.
Article in Pharmaceutical research, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.
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Who cites it
3 citing papers in PubMed, 18 citations in OpenAlex.
- Strategic approach to developing a self-microemulsifying drug delivery system to enhance antiplatelet activity and bioavailability of ticagrelor.International journal of nanomedicine · 2019Article
- The role of lipid-based nano delivery systems on oral bioavailability enhancement of fenofibrate, a BCS II drug: comparison with fast-release formulations.Journal of nanobiotechnology · 2014Article
- Directed self-assembled nanoparticles of probucol improve oral delivery: fabrication, performance and correlation.Pharmaceutical research · 2014Article
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeWe aimed to assess the fate of β-arteether lipid-based drug delivery systems (AE-LBDDS) in terms of resistance to lipolysis and permeation across intestinal cells.
methodsAE-LBDDS contained Tween 80 or Cremophor EL as surfactants, ethanol, Maisine 35-1 and vegetable oil. The solubilization behavior of AE was investigated during dynamic in vitro lipolysis. The permeation of AE-LBDDS was evaluated using Caco-2, HT29-MTX and M cell monolayers.
resultsA higher level of AE precipitation was observed for formulations containing Cremophor EL (~30%) compared to formulations containing Tween 80 (~10%) after lipolysis. However, rapid re-dissolution of the precipitated AE from LBDDS containing Cremophor EL in the intestinal biorelevant media was observed. The transport of AE loaded in LBDDS was enhanced in comparison to that of free drug due to the increased AE solubility. The apparent permeability of all AE-LBDDS across Caco-2 cell monolayers was approximately 3.10(-6) cm/s. A decrease in the permeability was observed at 4°C. M cells did not influence the transport of AE-LBDDS, and mucus decreased AE permeability when formulated with Tween 80. Furthermore, AE is not a P-glycoprotein substrate.
conclusionLBDDS that are partly resistant to in vitro lipolysis significantly increased the transport of AE across intestinal cell monolayers.
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