FORMULATION DEVELOPMENT AND CHARACTERIZATION : A STUDY
Ashish Kumar, Dr. Mahavir Chhajed
Page No. : 636-644
ABSTRACT
Bicalutamide (BIC) is a non-steroidal anti-androgen used for monotherapy in treating prostate cancer. It causes dose dependent reduction in the Prostate specific antigen (PSA) levels. It has the potential of working wonders at all the stages of prostate cancer disease continuum. BIC binds to cytoplasmic androgenic receptors and competitively inhibits the androgenic action by producing distortion of the co-activator binding site, thereby stopping the initiation of gene transcription. It causes some central androgen blockade and not much affects the testosterone and LH levels. It is also approved for combination therapy along with LHRH analogue for treating metastatic prostate cancer. It possesses a longer t1/2 and undergoes an extensive metabolism in liver.
Some of the major challenges currently faced by the current cancer treatment include the solubility and permeability limitations faced by most of the new chemical entities and anticancer agents. Another important challenge is reducing the side effects of the current chemotherapeutic treatment by aiming for tumour targeted therapy for cancer. The most recent advancement being “theranostics” in which simultaneous diagnosis and therapeutic treatment is possible by incorporating both the agents in a single carrier.
BIC comes under Biopharmaceutical classification system (BCS) Class II and suffers from solubility limitations, leading to dissolution and bioavailability issues. Thus, formulating a novel drug delivery system for this drug could open new avenues for increasing its effectiveness in prostate cancer treatment. To achieve this purpose a mesoporous silica nano delivery system was designed using MCM-41 carriers and thereafter functionalizing with ligands and surface moieties which help in achieving a targeted mesoporous system for the drug BIC.
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