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Pharma 2018
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E u r o p e a n C o n g r e s s o n
Pharma
A u g u s t 1 3 - 1 4 , 2 0 1 8
P a r i s , F r a n c e
American Journal of Pharmacology and Pharmacotherapeutics
ISSN: 2393-8862
M
any dispersion systems are currently in use as carriers of substances,
particularly biologically active compounds. Despite the great
advancements in the area of oral drug delivery systems, many drugs are prone
to poor oral bioavailability due to biological barriers that do not allow drug
penetration or metabolize the drug. Pro-nanoliposphere (PNL) is a type of self-
emulsifying delivery system, which can enhance the oral bioavailability of poorly
water soluble compounds by multiconcerted mechanisms which encompass
enhanced solubility of the incorporated drug. This formulation spontaneously
forms nanoparticles when gently mixed in an aqueous media, such as the upper
GI lumen content. When given orally, a drug is absorbed into the enterocytes
monolayer in the basolateral side of the intestine. From the apical side of the
enterocytes the drug is delivered via the portal vein to the liver and thereafter
into the systemic blood circulation. We developed oral formulations for some
insoluble drugs, like non psychotropic lipophilic phytocannabinoid cannabidiol
(CBD), with improved bioavailability using the PNL technology. Improved PNL
formulations were created using GRAS components which dissolved the drug
and enhance oral bioavailability. CBD shows therapeutic efficacy in various
indications. However, it has poor solubility and extensive Phase I and Phase II
metabolism at the enterocyte level, resulting in 6% oral bioavailability. The PNL
pre-concentrate with high load drug (50-150 mg per capsule), is composed of
lipidic and emulsifying excipients of GRAS status, upon addition to aqueous
media, such as stomach liquids, spontaneously form nano-droplets of 500
nm or below, preferably below 50 nm. The solvent, type of the triglyceride,
surfactants and their ratios are some of the most effective parameters. This
formulation possesses improved oral bioavailability when given to animal
or human. The liquid formulation can be packed in soft gelatine capsule or
absorbed in an absorbent to form semi-dry powder.
Biography
Eliyahu Shmoeli has completed his PhD fromTehran University.
He is a Post-doctoral fellow in the laboratory of Prof. Domb at
the Hebrew University of Jerusalem. He has published 8 papers
in reputed journals and contributed to a patent application.
Shmoeli.eliyahu@gmail.comPro-nanoliposphers (PNL) for improved oral bioavailability of
insoluble drugs
Eliyahu Shmoeli, Dvora Izgelov, Amnon Hoffman and Abraham
J Domb
Institute of Drug Research, The Hebrew University of Jerusalem, Israel
Eliyahu Shmoeli et al., Am J Pharmacol Pharmacother 2018, Volume 5
DOI: 10.21767/2393-8862-C1-003