Advances in Polymer Design for Enhancing Oral Drug Solubility and Delivery

Ting, Jeffrey; Porter, William A.; Mecca, Jodi M.; Bates, Frank S.; Reineke, Theresa M.

doi:10.1021/acs.bioconjchem.7b00646

Cited by 108 publications

(90 citation statements)

References 104 publications

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“…Nanoparticles (NPs), as a new generation of submicron-sized drug delivery systems, have the advantages of controlling drug release, avoiding drug degradation or leakage, good targeting, and improving bioavailability, among other advantages. Nanoparticle-based drug delivery systems are a research hotspot for new drug delivery technologies and new dosage forms [16].…”

Section: Introductionmentioning

confidence: 99%

Preparation of Puerarin Chitosan Oral Nanoparticles by Ionic Gelation Method and Its Related Kinetics

et al. 2020

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In this paper, as an active ingredient, puerarin chitosan nanoparticles (Pur-CS/TPP-NPs) are prepared by an ionic gelation method. The chitosan (CS) concentration, pH of the CS solution, sodium tripolyphosphate (TPP) concentration, stirring speed, stirring time, ultrasonic power, and dosage are used as single factors for investigation, and the encapsulation efficiency, drug loading capacity, particle size, and polydispersity index (PDI) are used as indicators for investigation. The optimal prescription is determined using the Box–Behnken effect surface design method. The characterization of the best formulation, which is determined via an in vitro release assay and liquid chromatography/tandem mass spectrometry (LC-MS/MS) analysis methods, is used here for pharmacokinetic studies. An in situ single-pass intestinal perfusion model is used to investigate drug absorption in the intestine. After characterization, the morphologies of the nanoparticles are intact. It can be seen from the in vitro release experiments that the equation fitted by the nanoparticles is the Higuchi model, the nanoparticle release process is very stable and without sudden release, indicating that the nanoparticles are well-released in vitro. The pharmacokinetic results and the in situ single-pass intestinal perfusion model study show that the bioavailability and absorption of Pur-CS/TPP-NPs were significantly higher than Pur. Thus, all the results show that the prepared nanoparticles can significantly improve the bioavailability of Pur, and we hope to lay the foundation for the development of new products of Pur.

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Section: Introductionmentioning

confidence: 99%

Preparation of Puerarin Chitosan Oral Nanoparticles by Ionic Gelation Method and Its Related Kinetics

et al. 2020

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“…With the structure of amphiphilic polymeric micelles, hydrophobic drug compounds are soluble within the hydrophobic nuclei, while the shell retains a hydration barrier that protects the integrity of each microcell [5,6]. As a result, polymeric micelles can be used as efficient containers for undesired solvents with low stability in physiological environments [7,8]. Additionally, the ability to categorize multiple groups provides a significant scope for accurately adjusting drug loading and drug-targeted propagation properties.…”

Section: Introductionmentioning

confidence: 99%

Biotin-functionalized copolymeric PEG-PCL micelles for in vivo tumour-targeted delivery of artemisinin

Nosrati

Barzegari

Danafar

et al. 2019

Artificial Cells, Nanomedicine, and Biotechnology

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Artemisinin is used as an antimalarial and anticancer agent with minimal toxic effects on the host body. Biotin-PEG-PCL polymers have been used for targeted drug delivery to cancer, as well as to improve the pharmacokinetics of the drug and reduce its effects. In this study, biotin-conjugated copolymers were fabricated with polymerization of the ring opening method and the properties of copolymer and nanoparticles were investigated using various techniques. The toxicity of artemisinin and its nanoparticles have been investigated on MCF-7 and normal HFF2 cells. The results showed that the encapsulation efficacy of artemisinin in nanoparticles was 45.5 ± 0.41%. The release profile of the drug indicates that the release is slow and controlled and is approximately pH dependent. The results of artemisinin cell culture on human breast cancer cells showed that biotin-PEG-PCL nanoparticles had an inhibitory effect on MCF-7 cells and had no toxic effects on HFF2 cells. Anticancer activity in vivo in the 4T1 breast cancer model showed that tumour volumes were decreased up 40 mm 3 by ART-loaded micelles and 76 mm 3 by free ART, compared to the control group (2150 mm). In vivo results showed that this formulation significantly increases the accumulation of substances in the tumours. Therefore, the molecular formulation of ART-based copolymers can be a desirable process for cancer treatment purposes.

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“…Typically, commercially available amorphous forms of APIs are prepared in conjunction with polymeric excipients, such as polyvinylpyrrolidone (PVP) and hydroxypropyl methylcellulose (HPMC), in order to prevent crystallization and increase bioavailability [ 15 , 45 , 46 , 47 ]. The amorphous form may be produced in a combined confinement and surface templating precipitation process, similar to the crystal forms that are the focus of this review, but it is more desirable to have molecular level mixing of the amorphous form with the polymer excipient for stability [ 48 , 49 , 50 , 51 ], so this is not a focus of the combined confinement and surface templating studies.…”

Section: Polymorphism In Pharmaceuticalsmentioning

confidence: 99%

“…Frequently, for class 2 and class 4 drugs (low solubility), the required clinical dosage of a drug is insoluble in physiological amounts of gastrointestinal fluid, rendering the drug inaccessible to the body [ 3 ]. According to the U.S. Pharmacopoeia, solubilities below 10 mg/mL are considered sparingly soluble and under 0.1 mg/mL are practically insoluble [ 3 , 15 , 16 ]. To dissolve some of these drugs such as piroxicam, a pain medication, over 2 L of GI fluid would be required [ 13 ].…”

Section: Introductionmentioning

confidence: 99%

Combining Surface Templating and Confinement for Controlling Pharmaceutical Crystallization

Banerjee

Brettmann

2020

Pharmaceutics

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Poor water solubility is one of the major challenges to the development of oral dosage forms containing active pharmaceutical ingredients (APIs). Polymorphism in APIs leads to crystals with different surface wettabilities and free energies, which can lead to different dissolution properties. Crystal size and habit further contribute to this variability. An important focus in pharmaceutical research has been on controlling the drug form to improve the solubility and thus bioavailability of APIs. In this regard, heterogeneous crystallization on surfaces and crystallization under confinement have become prominent forms of controlling polymorphism and drug crystal size and habits; however there has not been a thorough review into the emerging field of combining these approaches to control crystallization. This tutorial-style review addresses the major advances that have been made in controlling API forms using combined crystallization methods. By designing templates that not only control the surface functionality but also enable confinement of particles within a porous structure, these combined systems have the potential to provide better control over drug polymorph formation and crystal size and habit. This review further provides a perspective on the future of using a combined crystallization approach and suggests that combining surface templating with confinement provides the advantage of both techniques to rationally design systems for API nucleation.

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Advances in Polymer Design for Enhancing Oral Drug Solubility and Delivery

Cited by 108 publications

References 104 publications

Preparation of Puerarin Chitosan Oral Nanoparticles by Ionic Gelation Method and Its Related Kinetics

Preparation of Puerarin Chitosan Oral Nanoparticles by Ionic Gelation Method and Its Related Kinetics

Biotin-functionalized copolymeric PEG-PCL micelles for in vivo tumour-targeted delivery of artemisinin

Combining Surface Templating and Confinement for Controlling Pharmaceutical Crystallization

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