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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