Microenvironmental pH Modification in Buccal/Sublingual Dosage Forms for Systemic Drug Delivery

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems

Background:

• Many drug candidates exhibit poor water solubility, limiting their therapeutic efficacy.
• Buccal/sublingual drug delivery offers an alternative route for enhanced drug absorption.
• Microenvironmental pH (pH_M) modification is a key strategy to improve oral mucosal absorption of pH-dependent drugs.

Purpose of the Study:

• To introduce the concept of microenvironmental pH modification in buccal/sublingual dosage forms.
• To review saliva properties relevant to pH_M modification.
• To summarize suitable drug candidates, pH modifiers, measurement techniques, and challenges.

Main Methods:

• Literature review of pH_M modification strategies in buccal/sublingual formulations.
• Analysis of drug solubility, lipophilicity (Log D), and permeation.
• Evaluation of pH modifiers and measurement techniques.

Main Results:

• pH_M modification optimizes drug absorption by balancing solubility and permeation.
• Saliva properties play a crucial role in the effectiveness of pH_M modification.
• Careful selection of pH modifiers is necessary to mitigate risks like mucosal irritation and tooth erosion.

Conclusions:

• pH_M modification is a promising strategy for enhancing oral mucosal drug absorption.
• Formulation design must consider the interplay between drug properties, pH modifiers, and saliva.
• Further research is needed to address the challenges associated with pH_M modification.