Initial burst release

Initial burst release

Leuprolide acetate which is a highly active agonist of luteinizing hormone–releasing hormone (LH-RH) potently inhibits their secretion in the pituitary gland and it is useful in the treatment of hormone-dependent diseases in males and females. To eliminate the inconvenience of daily injection, Leuprolide acetate is available in the market, in the form of its depot for 1 month, 3 months, and 6 months, and depending upon the requirement of the patients, it is given as a parenteral solution.

To make this depot, one of the major and responsible ingredients required is Bioresorbable PLGA (Poly Lactic co glycolic acid) polymer, which is used to make microspheres of Leuprolide acetate along with this PLGA Polymer.

The higher level of free acid content in PLGA polymer causes an increase in the initial burst. If the free acid content is less than 0.1%, then the initial burst is less than 10%. These water-soluble acid fractions designated as free acid is ranging from heptamer to monomer/oligomer of lactic acid. These oligomers are assumed to interfere with the formation of the hydrophilic barrier by the arrangement of the polymer around the drug domains and increase the number of aqueous channels through the polymer barrier resulting in enhancement of the initial burst – called “tunnel effect”.

In order to have the quality of polymer i.e. free acid value in control, among all available in the market, Nomisma Healthcare Pvt. Ltd has produced PLGA polymers with optimum low-level free acid content value to control initial burst.

Factors affecting drug release

Factors affecting drug release

The drug release from the Leuprolide acetate depot mainly depends on the hydrolysis or degradation of PLGA (Poly lactic Co Glycolic acid) polymer involving diffusion and/or erosion either from its surface or from the mass.

The initial burst also depends upon the drug structure, drug concentration, hydrophilicity, or hydrophobicity.

According to solubility and water penetration into the polymer matrix, the drug on the surface in contact with the medium releases itself.

Random splitting of PLGA reduces molecular polymer weight considerably, but there is no considerable weight loss or soluble monomer substance.

The drug is gradually released through the second level’s thicker depleted sheet.

In the matrix, the polymer hydrolyzed into soluble monomeric and oligomeric components.

It permits the passage of a drug for release by erosive and diffusive processes prior to total polymer solvation.

The drug class also significantly contributes to the aqueous process’ matrix formation.

Prostate Cancer Cure is Possible

Prostate Cancer Cure is Possible

The prostate gland is an organ in reproductive anatomy. This small gland sits directly below the bladder and plays a role in producing seminal fluid, which is a component of semen. It also plays a role in hormone production and helps regulate urine flow. Changes in the prostate gland can lead to urinary problems.

Prostate problems are common, especially in older men. The most common include an inflamed prostate, an enlarged prostate, and prostate cancer.

Prostate cancer is the most common form of cancer in males after skin cancer. It affects around 1 in 8 males during their lifetime.

On average, people receive a prostate cancer diagnosis at age after 50.

To cure prostate cancer, one of the medicines approved by the FDA is Leuprolide acetate and its depot injection.

In the depot content, one of the major components commonly used is Biodegradable Polymer Namely Poly-lactic co-glycolic acid.

Across the globe, there are very few manufacturers who make this polymer and supply it to pharma industries for the same.

Nomisma Healthcare Pvt. Ltd. based in INDIA is one the commercial manufacturer of Biodegradable Polymer Poly-lactic co-glycolic acid to cater to pharma industries across the globe.