Pharmaceutical compatibility of dexamethasone with excipients commonly used in solid oral dosage forms

Santos, Widson Michael dos; Nóbrega, Fernanda Pontes; Andrade, Jéssica; Almeida, Lucas Ferreira de; Conceição, Marta Maria da; Medeiros, Ana Cláudia Dantas de; Medeiros, Francinalva Dantas de

doi:10.1007/s10973-020-09753-1

Cited by 13 publications

(3 citation statements)

References 47 publications

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“…The DSC thermogram of PLGA exhibited an endothermic peak at 50 °C depicting its glass transition temperature [ 30 ]. The thermal behavior of DEX was characterized by an endothermic peak at 255 °C, which is attributed to the melting point of the crystalline drug [ 31 , 32 ]. As shown in Figure 3 , no endothermic melting peak was determined for DEX NPs, which may be because DEX was dispersed at a molecular state within the nanoparticles in an amorphous or disordered crystalline state [ 33 ].…”

Section: Resultsmentioning

confidence: 99%

Rapidly Dissolving Microneedles for the Delivery of Steroid-Loaded Nanoparticles Intended for the Treatment of Inflammatory Skin Diseases

Dawud

Ammar

2023

Pharmaceutics

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Drug delivery through the skin has immense advantages compared to other routes of administration and offers an optimal way to treat inflammatory skin diseases, where corticosteroids are the cornerstone of topical therapy. Still, their therapeutic efficiency is limited due to inadequate skin permeability, potential side effects, and reduced patient compliance. To overcome these drawbacks, we propose a drug delivery system consisting of dexamethasone (DEX)-loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) incorporated in sodium alginate (SA) microneedles (MNs) as a minimally invasive dosage form for controlled drug release. Drug-loaded PLGA NPs were prepared by a nanoprecipitation method with a high encapsulation yield. They exhibited a controlled release pattern over 120 h. A modified vacuum-deposition micromolding method was used to load the obtained DEX-NPs into the tips of dissolving MNs. The NP-MNs showed improved insertion capabilities into the skin-simulant parafilm model and enhanced mechanical strength when tested against different static forces compared to their counterparts (SA-MNs). The results of an MN dissolution study following application to ex vivo chicken skin and agarose gel indicate that the NP-loaded segments of MNs dissolve within 15 s, in which the NPs are released into the skin. Taken together, the incorporation of DEX-NPs into SA-MNs could be a promising approach to bypass the limitations of conventional topical treatment of skin diseases, allowing for self-administration, increased patient compliance, and controlled drug release.

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Section: Resultsmentioning

confidence: 99%

Rapidly Dissolving Microneedles for the Delivery of Steroid-Loaded Nanoparticles Intended for the Treatment of Inflammatory Skin Diseases

Dawud

Ammar

2023

Pharmaceutics

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“…Since the further degradation products related to the peaks appeared after intensive thermal treatment were not identified in this study, their chemical structure and the mechanism of degradation starting from DEX with OXO as a possible intermediate is not clear. According to the literature, onset temperatures for mass loss of DEX are reported between 210 °C and 256.6 °C from TGA studies ( Santos et al, 2021 ; Oliveira et al, 2018 ; Jain and Datta, 2015 ). These temperatures are higher than the temperatures at which degradation products were identified in this study during the thermal stress test or HME.…”

Section: Discussionmentioning

confidence: 99%

Stability of Dexamethasone during Hot-Melt Extrusion of Filaments based on Eudragit® RS, Ethyl Cellulose and Polyethylene Oxide

Domsta,

Boralewski,

Ulbricht

et al. 2024

International Journal of Pharmaceutics: X

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“…It may also be feasible that dexamethasone dissolves in the elastic state of the polymer after glazing. Other authors have noted the thermal interactions of PVP with API, in the cases, for example of lipoic acid, diethylcarbamazine citrate and kaempferol [33].…”

Section: Multivariate Analysis Of Thermal Datamentioning

confidence: 99%

A combined differential scanning calorimetry and thermogravimetry approach for the effective assessment of drug substance-excipient compatibility

Rojek

Wesołowski

2022

J Therm Anal Calorim

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Differential scanning calorimetry (DSC) is a tool particularly recommended for rapid compatibility screening between active pharmaceutical ingredients (APIs) and excipients, whereas thermogravimetric analysis (TGA), a complementary technique to DSC, is primarily used to assess the thermal stability of APIs and excipients. Both DSC and TGA data can be converted using multivariate statistical methods, which are profitable tools in the detection of compatibility between ingredients. Principal component analysis (PCA) enables identification of compatibility by grouping samples into two clusters in a PCA score plot: acetazolamide and mixture with its highest content, and optionally a 1:1 mixture form one cluster, excipient and mixture with its highest quantity, and optionally a 1:1 mixture the second. Any variation from the arrangement of samples in the abovementioned clusters indicates incompatibility. By using cluster analysis, compatibility can be determined by four clusters, the first consisting of API, the second of groups mixture at the ratio of 7:3 and the third of two mixtures at ratios of 3:7 and 1:1, with the excipient in the remaining fourth cluster. Generally, the combination of DSC and TGA techniques with advanced statistical methods is favorable for the qualitative assessment of compatibility in acetazolamide mixtures with excipients such as mannitol, meglumine, lactose, magnesium stearate, β-cyclodextrin, chitosan, methylcellulose, starch 1500 and PVP K-30. In addition, PXRD revealed that acetazolamide retains its crystalline form after mixing. Accordingly, incompatibilities in acetazolamide mixtures can be attributed to chemical reactions.

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Pharmaceutical compatibility of dexamethasone with excipients commonly used in solid oral dosage forms

Cited by 13 publications

References 47 publications

Rapidly Dissolving Microneedles for the Delivery of Steroid-Loaded Nanoparticles Intended for the Treatment of Inflammatory Skin Diseases

Rapidly Dissolving Microneedles for the Delivery of Steroid-Loaded Nanoparticles Intended for the Treatment of Inflammatory Skin Diseases

Stability of Dexamethasone during Hot-Melt Extrusion of Filaments based on Eudragit® RS, Ethyl Cellulose and Polyethylene Oxide

A combined differential scanning calorimetry and thermogravimetry approach for the effective assessment of drug substance-excipient compatibility

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