Microenvironmental pH modifying films for buccal delivery of saquinavir: Effects of organic acids on pH and drug release in vitro

He, Shaolong; Østergaard, Jesper; Ashna, Madina; Nielsen, Carsten Uhd; Jacobsen, Jette Bredahl

doi:10.1016/j.ijpharm.2020.119567

Cited by 12 publications

(10 citation statements)

References 29 publications

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“…In one of our previous works, an UV/Vis imaging method with an agarose hydrogel mimicking the fluid on the surface of the buccal mucosa was constructed. The effect of the malic acid dose on the pH M during the initial dissolution of the buccal films, and the information related to film the swelling and possible drug precipitation in the films were monitored using this method [ 58 ]. The schematic view of the UV/Vis imaging setup is shown in Figure 4 .…”

Section: Methods For Microenvironmental Ph Measurementmentioning

confidence: 99%

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

He¹,

2023

Pharmaceutics

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Many drug candidates are poorly water-soluble. Microenvironmental pH (pHM) modification in buccal/sublingual dosage forms has attracted increasing interest as a promising pharmaceutical strategy to enhance the oral mucosal absorption of drugs with pH-dependent solubility. Optimizing drug absorption at the oral mucosa using pHM modification is considered to be a compromise between drug solubility and drug lipophilicity (Log D)/permeation. To create a desired pHM around formulations during the dissolution process, a suitable amount of pH modifiers should be added in the formulations, and the appropriate methods of pHM measurement are required. Despite pHM modification having been demonstrated to be effective in enhancing the oral mucosal absorption of drugs, some potential risks, such as oral mucosal irritation and teeth erosion caused by the pH modifiers, should not been neglected during the formulation design process. This review aims to provide a short introduction to the pHM modification concept in buccal/sublingual dosage forms, the properties of saliva related to pHM modification, as well as suitable drug candidates and pH modifiers for pHM modifying buccal/sublingual formulations. Additionally, the methods of pHM measurement, pHM modification methods and the corresponding challenges are summarized in the present review.

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Section: Methods For Microenvironmental Ph Measurementmentioning

confidence: 99%

Section: Figurementioning

confidence: 99%

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

He¹,

2023

Pharmaceutics

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“…Mechanical bonds are physical interactions relating to the penetration of mucoadhesive polymer Lipid matrix between the extracellular space act as an important barrier for the paracellular pathway, especially for high molecular weight compounds. Recently, [20] revealed the increase in drug release from the buccal films at lower pH attributed to the faster release characteristics of organic acid from the buccal films. Further, the ability of a drug to penetrate the oral mucosa depends on the lipid solubility, denoted by the oil/water partition coefficient [21].…”

Section: Mucoadhesion Theoriesmentioning

confidence: 99%

Mucoadhesive Delivery System: A Smart Way to Improve Bioavailability of Nutraceuticals

Subramanian

2021

Foods

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The conventional oral administration of many nutraceuticals exhibits poor oral bioavailability due to the harsh gastric conditions and first-pass metabolism. Oral mucosa has been recognized as a potential site for the delivery of therapeutic compounds. The mucoadhesive formulation can adhere to the mucosal membrane through various interaction mechanisms and enhance the retention and permeability of bioactive compounds. Absorption of bioactive compounds from the mucosa can improve bioavailability, as this route bypasses the hepatic first-pass metabolism and transit through the gastrointestinal tract. The mucosal administration is convenient, simple to access, and reported for increasing the bioactive concentration in plasma. Many mucoadhesive polymers, emulsifiers, thickeners used for the pharmaceutical formulation are accepted in the food sector. Introducing mucoadhesive formulations specific to the nutraceutical sector will be a game-changer as we are still looking for different ways to improve the bioavailability of many bioactive compounds. This article describes the overview of buccal mucosa, the concept of mucoadhesion and related theories, and different techniques of mucoadhesive formulations. Finally, the classification of mucoadhesive polymers and the mucoadhesive systems designed for the effective delivery of bioactive compounds are presented.

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“…He et al designed HPMC-based buccal films containing the basic drug saquinavir (pKa 7.1). With the aim of increasing the pH dependent solubility and release of saquinavir, the organic acids malic acid, citric acid or succinic acid were incorporated into the film matrix (242). In vitro release testing at pH 6.8 showed that addition of an organic acid increased the release of saquinavir from the buccal films.…”

Section: Miscellaneous Formulationsmentioning

confidence: 99%

“…Saquinavir release from the films was initiated by placing the films on the gel in the imaging system. The local pH, or microenvironmental pH, was assessed by imaging at 610 nm where bromothymol blue has a pH dependent absorbance (242). The apparent transient pH changes were the result of drug and excipient transport processes and the buffer capacity of the system.…”

Section: Miscellaneous Formulationsmentioning

confidence: 99%

Application of UV dissolution imaging to pharmaceutical systems

Brown

Ward

Fazili

et al. 2021

Advanced Drug Delivery Reviews

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Microenvironmental pH modifying films for buccal delivery of saquinavir: Effects of organic acids on pH and drug release in vitro

Cited by 12 publications

References 29 publications

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

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

Mucoadhesive Delivery System: A Smart Way to Improve Bioavailability of Nutraceuticals

Application of UV dissolution imaging to pharmaceutical systems

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