This article highlights the various techniques and upcoming strategies which can be employed for the development of highly notorious BCS class IV drugs. Also, ideal systems for BCS class IV should produce a therapeutic concentration of the drug at reasonable dose volumes for intravenous administration. Ideal oral dosage forms should produce both a reasonably high bioavailability and low inter and intra subject variability in absorption. To be clinically effective these drugs require the development of a proper delivery system for both oral and per oral delivery. The importance of the formulation composition and design to successful drug development is especially illustrated by the BCS class IV case. The inherent hurdles posed by these drugs hamper their translation to actual market. Formulation and development of an efficacious delivery system for BCS class IV drugs are herculean tasks for any formulator. A decade back, extreme examples of class IV compounds were an exception rather than the rule, yet today many drug candidates under development pipeline fall into this category. Also, most of the class IV drugs are substrate for P-glycoprotein (low permeability) and substrate for CYP3A4 (extensive pre systemic metabolism) which further potentiates the problem of poor therapeutic potential of these drugs. Some of the problems associated include low aqueous solubility, poor permeability, erratic and poor absorption, inter and intra subject variability and significant positive food effect which leads to low and variable bioavailability. BCS class IV drugs (e.g., amphotericin B, furosemide, acetazolamide, ritonavir, paclitaxel) exhibit many characteristics that are problematic for effective oral and per oral delivery.
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May 2023
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