RX422: Complex injectable formulations

What are complex injectables?

Parenteral formulations where drug is combined with carrier system to influence drug delivery, release, or targeting

What type of drugs would you use modified parenteral formulations for?

Insoluble drugs

Controlled / sustained release

What are the 4 types of targeted delivery technologies?

Liposomes

Nanoparticles

Micelles

Dendrimers

What are the 4 rules for injectable products?

Soluble in compatible vehicle for IV

Insoluble drugs can only be given IM, SUBQ, or via implants

Drugs must be fully soluble

Oil vehicles cannot be injected IV unless formulated as O/W

What is the volume of prolonged release IM injectables?

2-5ml

What is the safety concern with prolonged IM release injectables?

Must avoid any vein or artery

• needs trained personnel

What is the volume of prolonged SUBQ release injectables?

1-2mL

What agents make SUBQ injections more painful?

Low viscosity

Hypertonic

What are major complex formulations?

Hydrophobic drug molecule is encapsulated in a complex to improve drug delivery

What type of complexes are used to formulate major complex formulations?

Cyclodextrin

What do cyclodextrin complexes do?

Delivers drug across membrane without permeation

What are the advantages of cyclodextrin formulations?

Enhance solubility, bioavailability, stability

Reduce tissue irritation, odor, and taste masking

What is the MOA of drugs dispersed in oily vehicles?

Drug dissolves in oil → oil remains at injection site → drug slowly partitions into aqueous tissue fluid

How do you provide intermediate and prolonged drug release of hydrophobic drugs?

Aqueous suspension

• Saturate solution with suspended solid particles of drug

How do you provide intermediate and prolonged drug release of hydrophilic drugs?

Aqueous suspension

• Form long-chain fatty acid esters to make it dissolve slowly at injection site

What excipient will you see in aqueous suspensions?

Glycerin

What is the use of nanoparticles?

Targeting but sometimes used for controlled release

What are the 4 sites implants are being implamented?

Brain

Eye

SubQ

V*gina

What are In situ forming implants?

Thermally induced gelling systems

What disease state are in situ forming implants being used in?

Cancer