Trans-mucosal drug delivery means the needle-free drug
administration, where the drug has to reach and pass a mucus in order to
penetrate finally a tight epithelial layer. Trans-mucusol dosage form is thus
a generalized term for per-oral, nasal, pulmonal, buccal, sublingual and
vaginal dosage forms.
Examples of drugs to be
delivered by A-fects™:
Peptides / peptide hormones: Vasopressin; Desmopressin; Octreotide; Lanreotide;
Buserelin; Oxytocin; Decapeptyl; Carbetocin; Fertirelin; FSH; GnRH; HCG;
Levothyroxin; LH; Liothyronin;
poorly soluble drugs: 2,6-diisopropylphenol; amphotericin B; atovaquone; butorphanol base;
camptothecin; carbamazepin; carbendazim; clofazimine; cyclosporin A; danazol;
dexamethasone; diflunisal; domperidone; etoposide; hydrocortisone base;
ibuprofen; isradipine-darodipine; itraconazole; ketoprofen; loperamide
hydrochloride; meclizin; meclizin dihydrochloride; mitotane (o,p'-DDD);
piposulfan; piritramide; piroxicam; triamcinolone acetonide; vitamin K1-
phytomenadione;
penetration enhancer: Also known as permeability enhancer: Co-solvents
such as ethanol; DMSO; even water act as benetration enhancer; amphiphilc
molecules such as ionic detergents (cholate and its derivatives;
sulfobetaines) and non-ionic detergents (Tween; Brij). Fatty acids;
phospholipids.
The site of administration is for the
per-oral; gastro-intestinal; buccal; sublingual application the mouth. For
the nasal and pulmonal drug delivery way the nostrils are the site of
application.
The site of systemic uptake
is the epithelial cell-layer, covered by the protecting mucus. It is hydrated
by body fluids (tears (ocular); saliva (mouth); digestive juice (intestinum);
acid (gastric))
Co-encapsulation: The drug and/or the penetration enhancer are co-localized in the
drug delivery vehicle. Both are ether part of the liposomal membrane, or both are localized in the aqueous interion of the liposome as
water-soluble monomers, or both are localized in the aqueous interior of the
liposome as solid particle which is re-dissolved at or close to the site of
systemic entry.
A-fect™ tetraether lipids
A-fectsTM are a new type
of liposomes containing membrane spanning lipids derived from archaebacteria.
These new liposomes are superior to conventional liposomes in many respects.
As archaebacteria thrive in extreme environments e.g. extremely high or low
temperatures, highly acidic or basic milieu, archae-lipids are chemically
stable over a much greater range of temperatures and pH conditions compared
to conventional lipids. This presents a significant advancement for the
delivery of therapeutics, allowing for more varied routes of administration,
especially the oral route. Bernina has developed a variety of archae-lipids, uncharged as well as
positively or negatively charged, that accomplish the passage through the
GI-tract and facilitate the uptake of orally administered peptides. A set of
modified lipids mediating target specificity complements the highly variable A-fectTM toolbox.
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