Eutectic mixture and amorphous solid dispersion: Two different supersaturating drug delivery system strategies to improve griseofulvin release using saccharin

França, Maria Terezinha; Marcos, Tatyane Martins; Costa, Paulo F.A.; Bazzo, Giovana Carolina; Nicolay, Rafael Pereira; Gerola, Adriana P.; Stulzer, Hellen Karine

doi:10.1016/j.ijpharm.2022.121498

Cited by 8 publications

(6 citation statements)

References 54 publications

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“…In an attempt to improve the poor solubility of NCEs, approaches such as modifying the structure–activity relationship (SAR) were tried during the preclinical development stage [ 4 ]. However, the use of these approaches on NCEs is often limited, due to the requirement of a lipophilic nature to bind biological targets or to cross biological membranes [ 5 ]. Therefore, this resulted in an increased number of poorly aqueous soluble NCEs in the preclinical development, posing a challenge during formulation development [ 6 ].…”

Section: Introductionmentioning

confidence: 99%

Recent Advances in Amorphous Solid Dispersions: Preformulation, Formulation Strategies, Technological Advancements and Characterization

et al. 2022

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Amorphous solid dispersions (ASDs) are among the most popular and widely studied solubility enhancement techniques. Since their inception in the early 1960s, the formulation development of ASDs has undergone tremendous progress. For instance, the method of preparing ASDs evolved from solvent-based approaches to solvent-free methods such as hot melt extrusion and Kinetisol®. The formulation approaches have advanced from employing a single polymeric carrier to multiple carriers with plasticizers to improve the stability and performance of ASDs. Major excipient manufacturers recognized the potential of ASDs and began introducing specialty excipients ideal for formulating ASDs. In addition to traditional techniques such as differential scanning calorimeter (DSC) and X-ray crystallography, recent innovations such as nano-tomography, transmission electron microscopy (TEM), atomic force microscopy (AFM), and X-ray microscopy support a better understanding of the microstructure of ASDs. The purpose of this review is to highlight the recent advancements in the field of ASDs with respect to formulation approaches, methods of preparation, and advanced characterization techniques

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Section: Introductionmentioning

confidence: 99%

Recent Advances in Amorphous Solid Dispersions: Preformulation, Formulation Strategies, Technological Advancements and Characterization

et al. 2022

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“…Griseofulvin is an antifungal drug is employed to cure athlete's foot, ringworm, fungal infection, toenails, jock itch and fingernails. It is prescribed for onychomycosis, however, it has been mostly superseded by antifungals such as terbinafine, itraconazole, and fluconazole [9] …”

Section: Introductionmentioning

confidence: 99%

“…It is prescribed for onychomycosis, however, it has been mostly superseded by antifungals such as terbinafine, itraconazole, and fluconazole. [9] Mefenamic acid is used to relieve moderate to mild pain caused by a variety of disorders on a short-term basis. It is also used to reduce menstrual period pain and excessive bleeding.…”

Section: Introductionmentioning

confidence: 99%

Eutectic Mixtures to Enhance the Solubility of Active Pharmaceutical Ingredients: Density Functional Theory and Infrared Spectroscopy Approaches

et al. 2023

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The major issue with active pharmaceutical ingredients (APIs) is their slow dissolution rate and solubility. This makes them less likely to get into the body and less bioavailable. About 40 % of the drugs already on the market and 90 % being made have APIs that do not dissolve well in water. To deal with this problem, authors have designed eutectic mixture (EMs) of different drugs (danazol, griseofulvin, mefenamic acid, tolfenamic acid and tadalafil) with zinc chloride; studied their interaction and thermodynamic parameters using Density Functional Theory (DFT) computation. DFT calculations confirm an increase in the dipole moment of their EMs in comparison of APIs alone which increases the solubility. The change in Gibbs free energy of formation of EMs in the gaseous phase shows their feasibility ans stability.

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“…4,5 Amorphous drugs have higher apparent solubility than crystalline drugs. 6,7 The dispersion of solid carriers could increase the dissolution surface area of drugs by improving the dissolution rate of waterinsoluble drugs as well as their bioavailability, and this has good prospects for commercial development. 8,9 The widely used ASD carriers can be divided into polymer carriers and inorganic nanocarriers according to their physical properties and stability mechanisms.…”

Section: Introductionmentioning

confidence: 99%

“…Amorphous solid dispersion (ASD) refers to a single homogeneous dispersion system formed when drugs are highly dispersed in solid carriers in an amorphous form 4,5 . Amorphous drugs have higher apparent solubility than crystalline drugs 6,7 . The dispersion of solid carriers could increase the dissolution surface area of drugs by improving the dissolution rate of water‐insoluble drugs as well as their bioavailability, and this has good prospects for commercial development 8,9 .…”

Section: Introductionmentioning

confidence: 99%

Preparation of astaxanthin‐loaded composite micelles with coaxial electrospray technology for enhanced oral bioavailability and improved antioxidation capability

Liao,

Wang,

et al. 2023

J Sci Food Agric

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BackgroundAstaxanthin is approved by Food and Drug Administration (FDA) as a safe dietary supplement for humans. Astaxanthin, as a potent lipid‐soluble keto‐carotenoid, is widely used in food, cosmetics and pharmaceutical fields. However, the low solubility of astaxanthin limits its powerful biological activity and application in the aforementioned fields. This study aims to develop a delivery system to address the low solubility and bioavailability of astaxanthin and to enhance its antioxidant capacity.ResultsAstaxanthin‐loaded Composite Micelles were successfully prepared via Coaxial Electrospray Technology. Astaxanthin was existed in the amorphous state in the electro‐sprayed formulation with an approximate particle size of 186.28 nm with a polydispersity index of 0.243. In this delivery system, Soluplus and copovidone (PVPVA 64) were the main polymeric matrix for astaxanthin, which then released the drug upon contact with aqueous media, and results in an overall increase of drug solubility and a release rate of 94.08 %. Meanwhile, lecithin and PEG‐g‐CS could support the absorption of astaxanthin in the gastrointestinal tract and help the transmembrane transport. Consequently, the relative bioavailability reached about 308.33% and the ROS scavenging efficiency of formulation was 44.10 %, which was 1.57 times higher than that of free astaxanthin (28.10 %) when both were at the same concentration level based on astaxanthin.ConclusionIt could be deduced that coaxial electrospray could be applied to prepare a composite micelles system for the delivery of poorly water‐soluble active ingredients found in the fields of functional food, cosmetics and medicine.This article is protected by copyright. All rights reserved.

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Eutectic mixture and amorphous solid dispersion: Two different supersaturating drug delivery system strategies to improve griseofulvin release using saccharin

Cited by 8 publications

References 54 publications

Recent Advances in Amorphous Solid Dispersions: Preformulation, Formulation Strategies, Technological Advancements and Characterization

Recent Advances in Amorphous Solid Dispersions: Preformulation, Formulation Strategies, Technological Advancements and Characterization

Eutectic Mixtures to Enhance the Solubility of Active Pharmaceutical Ingredients: Density Functional Theory and Infrared Spectroscopy Approaches

Preparation of astaxanthin‐loaded composite micelles with coaxial electrospray technology for enhanced oral bioavailability and improved antioxidation capability

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