Non-steroidal anti-inflammatory drugs (NSAIDs) are one of the most commonly used and therapeutically effective groups of drugs in the medicinal field. They suppress inflammation in a similar way as steroids. They are also better than steroids in such a way that they cause fewer side effects of sedation, addiction and respiratory depression. NSAIDs act by inhibiting cyclooxygenase (COX) enzymes, COX-1 and COX-2. This type of inhibition results in reduced productions of precursors such as thromboxane, prostaglandin and leukotriene that are involved in the inflammatory pathways.

NSAIDs are poorly water-soluble drugs.Often, they are microencapsulated using the emulsion solvent diffusion method to modify and retard drug release from pharmaceutical dosage form. Further, encapsulation of NSAIDs into polymeric nanoparticles, followed by their encapsulation into polymeric microparticles has proved to reduce the release rate and suppress the undesired initial burst.

For instance, Ibuprofen-loaded PCL (Poly-epsilon-caprolactone) nanoparticles inside ethylcellulose/Eudragit RS polymeric microparticles, was successfully encapsulated, which effectively exhibited a control of both the release rate and burst effect. Ibuprofen, an NSAID, was selected as the model drug in this study. The low solubility (0.03-2.5mg/ml) and short plasma half-life of approximately 2 hours of Ibuprofen makes it an ideal choice to prepare a controlled release dosage form.

 Ibuprofen is commonly used to relieve the symptoms of mild and moderate pain and inflammation in conditions such as migraine, dental pain, dysmennorhea, headaches, back pain, muscular pain, rheumatic pain, cold and flu symptoms. Also, it is used to treat chronic diseases such as rheumatoid arthritis in which a controlled release dosage form is desired for symptom relief.

Although parenteral Ibuprofen formulation has been produced recently, there is no controlled release dosage form available in the pharmaceutical market. Considering that Ibuprofen is a anti-inflammatory agent used widely, this study of preparation of a biodegradable and controlled release parenteral Ibuprofen dosage form, based on nanoparticles will definitely of great interest.

Therapeutic Uses of PLGA Polymers in Contemporary Clinical Formulations

The use of the PLGA polymer for the development of new parenteral controlled drug delivery dosage forms appears to be very promising. Nanospheres with various release patterns can be prepared by altering the polymer species, molecular weight or monomer mixing ratio. FDA has approved PLGA for a number of medical applications.

 For instance, Lupron Depot, a controlled release formulation for treatment of advanced prostate cancer, was the first PLGA product cleared by FDA The effective dose this formulation, which contains leuprolide acetate encapsulated in biodegradable microspheres of 75:25 lactide/glycolide polymer, was reduced 1/4 – 1/8 of that required in the conventional drug formulation.

Another successful development of controlled drug delivery systems includes anticancer drug, Doxorubicin formulated into PLGA nanoparticles that exhibited controlled release over 1 month. In the following research work, Ibuprofen loaded PLGA nanoparticles are intended to be prepared with a view to possess the identical desired controlled release properties.

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Regards

Mary Wilson

Editorial office

Clinical Pharmacology and Toxicology Research

E-mail: pharmatoxicol@eclinicalsci.com