A therapeutic formulation comprising a
microemulsion of a therapeutic agent in free and / or conjugatively coupled form, wherein the
microemulsion comprises a water-in-oil (w / o)
microemulsion including a lipophilic phase and a hydrophilic phase, and has a hydrophilic and lipophilic balance (HLB) value between 3 and 7, wherein the therapeutic agent may for example be selected from the group consisting of
insulin,
calcitonin, ACTH,
glucagon,
somatostatin, somatotropin,
somatomedin, parathyroid honnone,
erythropoietin, hypothalamic releasing factors,
prolactin,
thyroid stimulating hormones, endorphins, enkephalins,
vasopressin, non-naturally occurring opioids,
superoxide dismutase,
interferon,
asparaginase,
arginase,
arginine deaminease,
adenosine deaminase,
ribonuclease,
trypsin,
chymotrypsin,
papain, Ara-A (Arabinofuranosyladenine), Acylguanosine, Nordeoxyguanosine, Azidothym id ine, Didesoxyadenosine, Dideoxycytidine, Dideoxyinosine Floxuridine, 6-
Mercaptopurine,
Doxorubicin,
Daunorubicin, or I-darubicin,
Erythromycin,
Vancomycin, oleandomycin,
Ampicillin;
Quinidine and
Heparin. In a particular aspect, the invention comprises an
insulin composition suitable for parenteral as well as non-parenteral administration, preferably oral or parenteral administration, comprising
insulin covalently coupled with a
polymer including (i) a linear polyalkylene glycol
moiety and (ii) a lipophilic
moiety, wherein the insulin, the linear polyalkylene glycol
moiety and the lipophilic moiety are conformationally arranged in relation to one another such that the insulin in the composition has an enhanced
in vivo resistance to
enzymatic degradation, relative to insulin alone. The microemulsion compositions of the invention are usefully employed in therapeutic as well as non-therapeutic, e.g., diagnostic, applications.