Challenges to improve the biopharmaceutical properties of poorly water-soluble drugs and the application of the solid dispersion technology

Tambosi, Gabriela; Coelho, Paola Felippi; Soares, Luciano; Lenschow, Iára Cristina Schmücker; Zétola, Melissa; Stulzer, Hellen Karine; Pezzini, Bianca Ramos

doi:10.1590/s1517-707620180004.0558

Cited by 36 publications

(31 citation statements)

References 44 publications

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“…There are excellent reviews and research papers published so far [ 9 , 11 , 12 , 13 , 14 , 15 , 16 , 17 , 18 ], regarding the stability of amorphous drugs as well as insoluble drug delivery strategies. Selection of proper and suitable polymers, their miscibility, and interactions with a drug are favored approaches.…”

Section: Introductionmentioning

confidence: 99%

Thermal Stability of Amorphous Solid Dispersions

Jelić¹

2021

Molecules

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Amorphous solid dispersion drug delivery systems (ASD DDS) were proved to be efficient for the enhancement of solubility and bioavailability of poorly water-soluble drugs. One of the major keys for successful preparation of ASD is the selection of appropriate excipients, mostly polymers, which have a crucial role in improving drug solubility and its physical stability. Even though, excipients should be chemically inert, there is some evidence that polymers can affect the thermal stability of active pharmaceutical ingredients (API). The thermal stability of a drug is closely related to the shelf-life of pharmaceutical products and therefore it is a matter of high pharmaceutical relevance. An overview of thermal stability of amorphous solids is provided in this paper. Evaluation of thermal stability of amorphous solid dispersion is perceived from the physicochemical perspective, from a kinetic (motions) and thermodynamic (energy) point of view, focusing on activation energy and fragility, as well all other relevant parameters for ASD design, with a glance on computational kinetic analysis of solid-state decomposition.

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Section: Introductionmentioning

confidence: 99%

Thermal Stability of Amorphous Solid Dispersions

Jelić¹

2021

Molecules

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“…6 The properties and features of such solid dispersions of drugs are affected by various factors, such as the preparation method and the type of the carrier used. [7][8][9] And the number of water-soluble carrier materials, especially PEG 10 or PVP 11 have gained attention for this purpose. One of the most useful techniques in pharmaceutical engineering that are used to make spherical drug crystals which are small in size, uniform and have narrow distribution, is the spray drying technique.…”

Section: Introductionmentioning

confidence: 99%

Spray Dried Amorphous Form of Simvastatin: Preparation and Evaluation of the Buccal Tablet

Sreeharsha¹,

Hiremath²,

Sarudkar³

et al. 2019

IJPER

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Background: The success of a drug primarily depends on its bioavailability. By enhancing the solubility and dissolution properties of drugs that are scarcely water soluble, significantly improves their bioavailability. Methods: This study was aimed to prepare a solid dispersion of the drug simvastatin that is a poorly water-soluble drug, through the spray drying technique. Solid dispersion carrier PVP, adsorbent Aerosil 200 and solvent dichloromethane were used to prepare solid dispersion. The pure simvastatin, solid dispersion and physical mixture were analyzed using FTIR, XRD and DSC studies. IR studies confirmed the possibility of hydrogen bonding in solid dispersion. Results: XRD and DSC studies revealed that the amorphous form of simvastatin was present in the solid dispersion. The spray dried form of simvastatin was formulated into a buccal tablet by using carbopol 934 and HPMC K4M as mucoadhesive polymers. The drug release from buccal tablets indicated that improvement in solubility, the rate of dissolution of poorly water-soluble drug simvastatin. Conclusion: The study shows that the tremendous potential of solid dispersions of simvastatin by using spray drying technique.

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“…Drug bioavailability is a major concern for the therapeutic efficacy of anticancer drugs. 17,18 Investigation suggests that nanoparticles are a promising tool for enhancement of cancer treatment because of their bioavailability enhancement property. 19 Nanoparticles are reported to enhance the bioavailability of less water-soluble drugs and prevent their degradation from various environmental factors.…”

Section: Introductionmentioning

confidence: 99%

Evaluation of Antitumor Efficacy of Chitosan-Tamarind Gum Polysaccharide Polyelectrolyte Complex Stabilized Nanoparticles of Simvastatin

Malviya

Raj

Fuloria

et al. 2021

IJN

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The present study was intended to fabricate chitosan (Ch)-tamarind gum polysaccharide (TGP) polyelectrolyte complex stabilized cubic nanoparticles of simvastatin and evaluate their potential against human breast cancer cell lines. Materials and Methods: The antisolvent precipitation method was used for formulation of nanoparticles. Factorial design (3 2 ) was utilized as a tool to analyze the effect of Ch and TGP concentration on particle size and entrapment efficiency of nanoparticles. Results: Formulated nanoparticles showed high entrapment efficiency (67.19±0.42-83.36 ±0.23%) and small size (53.3-383.1 nm). The present investigation involved utilization of two biological membranes (egg and tomato) as biological barriers for drug release. The study revealed that drug release from tomato membranes was retarded (as compared to egg membranes) but the release pattern matched that of egg membranes. All formulations followed the Baker-Lansdale model of drug release irrespective of the two different biological barriers. Stability studies were carried out for 45 days and exhibited less variation in particle size as well as a reduction in entrapment efficiency. Simvastatin loaded PEC stabilized nanoparticles exhibited better control on growth of human breast cancer cell lines than simple simvastatin. An unusual anticancer effect of simvastatin nanoparticles is also supported by several other research studies. Conclusion:The present study involves first-time synthesis of Ch-TGP polyelectrolyte complex stabilized nanoparticles of simvastatin against MCF-7 cells. It recommends that, in future, theoretical modeling and IVIVC should be carried out for perfect designing of delivery systems.

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Challenges to improve the biopharmaceutical properties of poorly water-soluble drugs and the application of the solid dispersion technology

Cited by 36 publications

References 44 publications

Thermal Stability of Amorphous Solid Dispersions

Thermal Stability of Amorphous Solid Dispersions

Spray Dried Amorphous Form of Simvastatin: Preparation and Evaluation of the Buccal Tablet

Evaluation of Antitumor Efficacy of Chitosan-Tamarind Gum Polysaccharide Polyelectrolyte Complex Stabilized Nanoparticles of Simvastatin

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