Degradation Pathways

Loftsson, Þorsteinn

doi:10.1016/b978-0-12-411548-4.00003-9

Cited by 6 publications

(3 citation statements)

References 31 publications

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“…Due to its known instability, NM degradation was controlled to minimize burn variability between groups. The administration buffer was prepared at a pH high enough that aziridinium ring formation occurs (above pH 3), but low enough to minimize degradation (as close to pH 3 as possible) 29 . An acetate buffer (0.1 M, pH 4.0) was used as a vehicle for NM administration.…”

Section: Methodsmentioning

confidence: 99%

Depilatory double‐disc mouse model for evaluation of vesicant dermal injury pharmacotherapy countermeasures

Roldan

Laskin

et al. 2023

Anim Models and Exp Med

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Background Sulfur mustard (SM) is a chemical warfare vesicant that severely injures exposed eyes, lungs, and skin. Mechlorethamine hydrochloride (NM) is widely used as an SM surrogate. This study aimed to develop a depilatory double‐disc (DDD) NM skin burn model for investigating vesicant pharmacotherapy countermeasures. Methods Hair removal method (clipping only versus clipping followed by a depilatory), the effect of acetone in the vesicant administration vehicle, NM dose (0.5–20 μmol), vehicle volume (5–20 μl), and time course (0.5–21 days) were investigated using male and female CD‐1 mice. Edema, an indicator of burn response, was assessed by biopsy skin weight. The ideal NM dose to induce partial‐thickness burns was assessed by edema and histopathologic evaluation. The optimized DDD model was validated using an established reagent, NDH‐4338, a cyclooxygenase, inducible nitric oxide synthase, and acetylcholinesterase inhibitor prodrug. Results Clipping/depilatory resulted in a 5‐fold higher skin edematous response and was highly reproducible (18‐fold lower %CV) compared to clipping alone. Acetone did not affect edema formation. Peak edema occurred 24–48 h after NM administration using optimized dosing methods and volume. Ideal partial‐thickness burns were achieved with 5 μmol of NM and responded to treatment with NDH‐4338. No differences in burn edematous responses were observed between males and females. Conclusion A highly reproducible and sensitive partial‐thickness skin burn model was developed for assessing vesicant pharmacotherapy countermeasures. This model provides clinically relevant wound severity and eliminates the need for organic solvents that induce changes to the skin barrier function.

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Section: Methodsmentioning

confidence: 99%

Depilatory double‐disc mouse model for evaluation of vesicant dermal injury pharmacotherapy countermeasures

Roldan

Laskin

et al. 2023

Anim Models and Exp Med

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“…After epineural and neural diffusion, procaine reversibly and preferentially binds to active sites on the cytoplasmic aspect of neuronal voltage-gated sodium channels. [ 59 , 60 ] Ritonavir 5 µg in 1 mL at 25°C Antiretroviral Binding to HIV-1 protease, which causes cleavage of protein precursors generating new viral particles. Protease inhibitors disrupt this cleavage process, interrupting the production of new viral particles.…”

Section: Drug With Good Gfa (Ggfa Drug)mentioning

confidence: 99%

Characterization of Drug with Good Glass-Forming Ability Loaded Mesoporous Silica Nanoparticles and Its Impact Toward in vitro and in vivo Studies

Budiman,

Anastasya,

Handini

et al. 2024

IJN

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Solid oral dosage forms are mostly preferred in pharmaceutical formulation development due to patient convenience, ease of product handling, high throughput, low manufacturing costs, with good physical and chemical stability. However, 70% of drug candidates have poor water solubility leading to compromised bioavailability. This phenomenon occurs because drug molecules are often absorbed after dissolving in gastrointestinal fluid. To address this limitation, delivery systems designed to improve the pharmacokinetics of drug molecules are needed to allow controlled release and target-specific delivery. Among various strategies, amorphous formulations show significantly high potential, particularly for molecules with solubility-limited dissolution rates. The ease of drug molecules to amorphized is known as their glass-forming ability (GFA). Specifically, drug molecules categorized into class III based on the Taylor classification have a low recrystallization tendency and high GFA after cooling, with substantial “glass stability” when heated. In the last decades, the application of mesoporous silica nanoparticles (MSNs) as drug delivery systems (DDS) has gained significant attention in various investigations and the pharmaceutical industry. This is attributed to the unique physicochemical properties of MSNs, including high loading capacity, recrystallization inhibition, excellent biocompatibility, and easy functionalization. Therefore, this study aimed to discuss the current state of good glass former drug loaded mesoporous silica and shows its impact on the pharmaceutical properties including dissolution and physical stability, along with in vivo study. The results show the importance of determining whether mesoporous structures are needed in amorphous formulations to improve the pharmaceutical properties of drug with a favorable GFA.

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“…Combinations of two or more antioxidants have been shown to produce synergistic effects. For example, BHT, BHA and alkyl gallates are much more effective in the presence of citric, tartaric or phosphoric acids [12].…”

Section: Antioxidants and Chelating Agentsmentioning

confidence: 99%

Understanding Your Creams: Principles of Dermatological Formulation

2022

Clin Exp Dermatol Ther

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Traditionally in Medical and Dermatological training, the focus has been on the understanding, diagnosis and management of skin diseases, including treatment using topical formulations. With the exception of learning about the pharmacologically active ingredient, there is a neglect and gap in understanding the other ingredients that comprise a topical formulation, which is a prime tool in our therapeutic armamentarium. Such an understanding is essential to allow for skilful deployment of treatments, management of problems these applications can secondarily cause, and the formulation of more suitable agents for individual or commercial use. This article examines the composition of a topical product, including its active ingredient (s), common topical vehicles used for drug delivery, and additives, paying particular attention to how these ingredients interact with the skin for absorption and which of them are more likely to cause contact dermatitis.

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Degradation Pathways

Cited by 6 publications

References 31 publications

Depilatory double‐disc mouse model for evaluation of vesicant dermal injury pharmacotherapy countermeasures

Depilatory double‐disc mouse model for evaluation of vesicant dermal injury pharmacotherapy countermeasures

Characterization of Drug with Good Glass-Forming Ability Loaded Mesoporous Silica Nanoparticles and Its Impact Toward in vitro and in vivo Studies

Understanding Your Creams: Principles of Dermatological Formulation

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