A novel controlled drug delivery system based on pH-responsive hydrogels included in soft gelatin capsules

Frutos, G.; Prior-Cabanillas, Alberto; París, Rodrigo; Quijada‐Garrido, Isabel

doi:10.1016/j.actbio.2010.07.018

Cited by 47 publications

(30 citation statements)

References 36 publications

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“…However, in the cytoplasm, the red fluorescence of doxorubicin hydrochloride was the strongest, and that of doxorubicin was the weakest. The red fluorescence of doxorubicin-loaded mPEG 45 -PH 15 was comparable with that of doxorubicin-loaded mPEG 45 -PH 30 -PLLA 82 nanoparticles. Being a hydrophilic drug, doxorubicin hydrochloride was easily internalized in HepG2 cells and diffused into the nuclei.…”

Section: Resultsmentioning

confidence: 50%

“…36 The calculated critical aggregation concentrations of the mPEG 45 -PH 15 -PLLA 82 and mPEG 45 -PH 30 -PLLA 82 nanoparticles were 3 µg/mL and 8 µg/mL, respectively. This suggests that the nanoparticles with a shorter poly(L-histidine) chain length were more stable due to their lower critical aggregation concentration.…”

Section: Resultsmentioning

confidence: 99%

“…12,13 Stimulus-sensitive drug carriers could trigger drug release in response to local environmental conditions, so this is a potentially promising approach for cancer chemotherapy. Stimuli such as pH, [14][15][16][17] enzymes, 18 and temperature [19][20][21] have been reported to regulate the release of antitumor drugs. Because the pH in solid tumor tissue is lower than that in normal tissue, 22,23 pH-sensitive drug release is competitive and favorable for chemotherapy.…”

Section: Introductionmentioning

confidence: 99%

“…Stimuli such as pH, [14][15][16][17] and release drugs loaded into intracellular acidic endosomes. The other strategy is to induce physical dissociation [26][27][28][29][30] or interior structural change via variation in pH level.…”

Section: Introductionmentioning

confidence: 99%

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Effects of pH-sensitive chain length on release of doxorubicin from mPEG-b-PH-b-PLLA nanoparticles

Liu¹,

He²,

Liu³

et al. 2012

IJN

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Background: Two methoxyl poly(ethylene glycol)-poly(L-histidine)-poly(L-lactide) (mPEG-PH-PLLA) triblock copolymers with different poly(L-histidine) chain lengths were synthesized. The morphology and biocompatibility of these self-assembled nanoparticles was investigated. Methods: Doxorubicin, an antitumor drug, was trapped in the nanoparticles to explore their drug-release behavior. The drug-loaded nanoparticles were incubated with HepG2 cells to evaluate their antitumor efficacy in vitro. The effects of poly(L-histidine) chain length on the properties, drug-release behavior, and antitumor efficiency of the nanoparticles were investigated. Results: The nanoparticles were pH-sensitive. The mean diameters of the two types of mPEG-PH-PLLA nanoparticle were less than 200 nm when the pH values were 5.0 and 7.4. The nanoparticles were nontoxic to NIH 3T3 fibroblasts and HepG2 cells. The release of doxorubicin at pH 5.0 was much faster than that at pH 7.4. The release rate of mPEG 45 -PH 15 -PLLA 82 nanoparticles was much faster than that of mPEG 45 -PH 30 -PLLA 82 nanoparticles at pH 5.0. Conclusion:The inhibition effect of mPEG 45 -PH 15 -PLLA 82 nanoparticles on the growth of HepG2 cells was greater than that of mPEG 45 -PH 30 -PLLA 82 nanoparticles when the concentration of encapsulated doxorubicin was less than 15 µg/mL. Keywords: poly(ethylene glycol), poly(L-histidine), poly(L-lactide), pH sensitivity, doxorubicin, drug release, nanoparticle IntroductionBiodegradable polymeric nanoparticle-based antitumor drug delivery systems have attracted much interest among biomaterials scientists [1][2][3] for their advantages of excellent biocompatibility, escaping of the reticuloendothelial system to avoid blood clearance and elimination from the body, [4][5][6] and passive targeting to tumor cells due to the enhanced permeation and retention effect. [7][8][9][10][11] However, passive drug delivery systems cannot guarantee optimal therapeutic efficacy in tumors with multidrug resistance.12,13 Stimulus-sensitive drug carriers could trigger drug release in response to local environmental conditions, so this is a potentially promising approach for cancer chemotherapy. Stimuli such as pH, [14][15][16][17] and release drugs loaded into intracellular acidic endosomes. The other strategy is to induce physical dissociation [26][27][28][29][30] or interior structural change via variation in pH level. 31,32 The pKa of the imidazole group in L-histidine is around 6.0, which means that protonation would occur when pH is about 6.0. For polymeric nanoparticles containing poly(Lhistidine) segments, protonation of imidazole groups would lead to structural change in the nanoparticles, and this has been utilized to fabricate pH-sensitive nanodrug carriers. [26][27][28][29][30][31] In addition to protonation, the poly(L-histidine) segment has strong endosomolytic properties via its proton sponge effect and/or interaction with anionic phospholipids in the endosomal membrane 27,28,33 for easy delivery of drugs into cancer cells. In our prev...

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Section: Resultsmentioning

confidence: 50%

Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Effects of pH-sensitive chain length on release of doxorubicin from mPEG-b-PH-b-PLLA nanoparticles

Liu¹,

He²,

Liu³

et al. 2012

IJN

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“…It is known that gelatin is created through either acid or alkaline hydrolysis of collagen and has conventionally been employed for pharmaceutical, food, and cosmetic products. 36 The hydrolysis process hydrolyzes the amide structures of asparagine or glutamine side chains, generating a high percentage of carboxylic groups and amino groups, 37 which increases the hydrophilicity. So in this study, the antibacterial coating showed a higher hydrophilicity ( Figure 2B).…”

Section: Discussionmentioning

confidence: 99%

Antibacterial activity and biological performance of a novel antibacterial coating containing a halogenated furanone compound loaded poly(L-lactic acid) nanoparticles on microarc-oxidized titanium

Cheng¹,

Zhao²,

Liu³

et al. 2015

IJN

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Titanium implants have been widely used for many medical applications, but bacterial infection after implant surgery remains one of the most common and intractable complications. To this end, long-term antibacterial ability of the implant surface is highly desirable to prevent implant-associated infection. In this study, a novel antibacterial coating containing a new antibacterial agent, (Z-)-4-bromo-5-(bromomethylene)-2(5H)-furanone loaded poly(L-lactic acid) nanoparticles, was fabricated on microarc-oxidized titanium for this purpose. The antibacterial coating produced a unique inhibition zone against Staphylococcus aureus throughout a 60-day study period, which is normally long enough to prevent the infection around implants in the early and intermediate stages. The antibacterial rate for adherent S. aureus was about 100% in the first 10 days and constantly remained over 90% in the following 20 days. Fluorescence staining of adherent S. aureus also confirmed the excellent antibacterial ability of the antibacterial coating. Moreover, in vitro experiments showed an enhanced osteoblast adhesion and proliferation on the antibacterial coating, and more notable cell spread was observed at the early stage. It is therefore concluded that the fabricated antibacterial coating, which exhibits relatively long-term antibacterial ability and excellent biological performance, is a potential and promising strategy to prevent implant-associated infection.

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Shell Formulation in Soft Gelatin Capsules: Design and Characterization

Naharros‐Molinero,

Caballo‐González,

de la Mata

et al. 2023

Adv Healthcare Materials

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Soft gelatin capsules are the most widely used pharmaceutical form after tablets. The active components, active pharmaceutical ingredients or nutrients are dissolved or suspended in a liquid or semi‐solid fill, which is covered with a gelatin shell. Several factors can modify the properties of the gelatin shell and subsequently affect their operative handling during manufacturing process and the stability of the soft gelatin capsules. Three elements appear to be crucial: the shell formulation (type and content of the different components such as gelatin ‐source, extraction method‐, plasticizers, or additives); the manufacture and storage conditions (temperature, humidity, light) as well as the interactions between fill‐shell formulas. Mechanical and thermal analysis arise as straightforward but highly useful tools to monitor the properties of the gelatin shell. This review provides an updated overview on the shell formulation and design. Additionally, it presents the uses of mechanical and thermal techniques to characterize and evaluate the impact of different parameters on the gelatin behavior over the production and stability of these pharmaceutical forms. This will help to detect changes that are yet not visible by visual inspection ensuring a suitable finished product over its shelf‐life.This article is protected by copyright. All rights reserved

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A novel controlled drug delivery system based on pH-responsive hydrogels included in soft gelatin capsules

Cited by 47 publications

References 36 publications

Effects of pH-sensitive chain length on release of doxorubicin from mPEG-b-PH-b-PLLA nanoparticles

Effects of pH-sensitive chain length on release of doxorubicin from mPEG-b-PH-b-PLLA nanoparticles

Antibacterial activity and biological performance of a novel antibacterial coating containing a halogenated furanone compound loaded poly(L-lactic acid) nanoparticles on microarc-oxidized titanium

Shell Formulation in Soft Gelatin Capsules: Design and Characterization

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