Drug intelligence / Profile preview

diclofenac HPBCD

Development stage
Phase 3
Lead developer
IBSA
Modality
Small Molecules, Nanoparticles → Drug Delivery Systems
Administration
Subcutaneous, Intramuscular, Intravenous
01

Overview

Diclofenac HPBCD is a novel injectable formulation of the nonsteroidal anti-inflammatory drug (NSAID) diclofenac complexed with hydroxypropyl-β-cyclodextrin (HPβCD). This formulation enhances the solubility and bioavailability of diclofenac for parenteral administration (subcutaneous, intramuscular, intravenous), enabling rapid onset of analgesic action at lower doses compared to conventional formulations. The mechanism of action is inhibition of cyclooxygenase enzymes (COX-1 and COX-2), leading to reduced synthesis of prostanoids involved in pain and inflammation. The addition of HPβCD allows for effective pain management with potentially improved tolerability and safety profile due to lower required doses. It is primarily indicated for acute pain conditions such as postoperative pain, musculoskeletal pain, back pain, inflammatory pain, and renal colic[2][5][8][9].

Brand names
AkisDicloin
Other names
diclofenac hydroxypropyl-β-cyclodextrinHPβCD-diclofenacdiclofenac/HPβCD
02

Targets

PGHS-1 (Prostaglandin G/H Synthase 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)

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