New pH-Sensitive Hydrogels for Oral Delivery of Hydrophobic Drugs

Objective: This review article explores solid dispersions (SDs) as one of the suitable approaches to formulate poorly water-soluble drugs. The objective of this review on SD techniques is to explore their utility as a feasible, simple, and economically viable method for augmentation of dissolution of hydrophobic drugs. Methods: Various types of SDs are classified and compared. Use of surfactants to stabilize the SDs and their potential advantages and disadvantages has been discussed. Different techniques for preparing and evaluating SDs are appraised along with discussions on scalability and industrial production. Review of the current research on SD along with future trends is also offered. Results: Based on the various researches, SDs offer an efficient means of improving bioavailability while concurrently contributing to lower toxicity and dose-reduction. Conclusion: Solid-dispersions have been and continue to be one of the key technologies for solving the issue of poor solubility for newer hydrophobic molecules which are being discovered. This would give a new lease of life for such drugs enabling them to be delivered in an effective way.

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PLGA Nanoparticles for Oral Delivery of Hydrophobic Drugs: Influence of Organic Solvent on Nanoparticle Formation and Release Behavior In Vitro and In Vivo Using Estradiol as a Model Drug

Journal of Pharmaceutical Sciences ◽

10.1002/jps.21158 ◽

2008 ◽

Vol 97 (4) ◽

pp. 1530-1542 ◽

Cited By ~ 161

Author(s):

D.K. Sahana ◽

G. Mittal ◽

V. Bhardwaj ◽

M.N.V.Ravi Kumar

Keyword(s):

Organic Solvent ◽

Oral Delivery ◽

Plga Nanoparticles ◽

Hydrophobic Drugs ◽

Release Behavior ◽

Nanoparticle Formation ◽

Model Drug

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Electrospun poly(NVCL-co-AA) fibers as potential thermo-and pH-sensitive agents for controlled release of hydrophobic drugs

Materials Science and Engineering B ◽

10.1016/j.mseb.2021.115531 ◽

2022 ◽

Vol 276 ◽

pp. 115531

Author(s):

Marwa Sta ◽

Dayane B. Tada ◽

Simone F. Medeiros ◽

Amilton M. Santos ◽

Nicole R. Demarquette

Keyword(s):

Controlled Release ◽

Ph Sensitive ◽

Hydrophobic Drugs

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Intestine-penetrating, pH-sensitive and double-layered nanoparticles for oral delivery of doxorubicin with reduced toxicity

Journal of Materials Chemistry B ◽

10.1039/c9tb00212j ◽

2019 ◽

Vol 7 (23) ◽

pp. 3692-3703 ◽

Cited By ~ 6

Author(s):

Min Sun ◽

Dapeng Li ◽

Xin Wang ◽

Le He ◽

Xiaodong Lv ◽

...

Keyword(s):

Intestinal Absorption ◽

Oral Delivery ◽

Ph Sensitive ◽

Oral Toxicity ◽

Absorption Effect ◽

Reduced Toxicity

Herein, CMC-coated double-layered nanoparticles were prepared to induce the oral toxicity of doxorubicin via the intestinal absorption effect.

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A facile nanoaggregation strategy for oral delivery of hydrophobic drugs by utilizing acid–base neutralization reactions

Nanotechnology ◽

10.1088/0957-4484/19/37/375104 ◽

2008 ◽

Vol 19 (37) ◽

pp. 375104 ◽

Cited By ~ 22

Author(s):

Huabing Chen ◽

Jiangling Wan ◽

Yirui Wang ◽

Dongsheng Mou ◽

Hongbin Liu ◽

...

Keyword(s):

Oral Delivery ◽

Hydrophobic Drugs ◽

Acid Base

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Preparation andin vitroevaluation of new pH-sensitive hydrogel beads for oral delivery of protein drugs

Journal of Applied Polymer Science ◽

10.1002/app.30881 ◽

2010 ◽

Vol 115 (5) ◽

pp. 2828-2837 ◽

Cited By ~ 22

Author(s):

I. M. El-Sherbiny ◽

E. M. Abdel-Bary ◽

D. R. K. Harding

Keyword(s):

Oral Delivery ◽

Ph Sensitive ◽

Protein Drugs ◽

Hydrogel Beads ◽

Ph Sensitive Hydrogel

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A novel pH-sensitive interferon-β (INF-β) oral delivery system for application in multiple sclerosis

International Journal of Pharmaceutics ◽

10.1016/j.ijpharm.2013.08.038 ◽

2013 ◽

Vol 456 (2) ◽

pp. 459-472 ◽

Cited By ~ 19

Author(s):

Pierre P.D. Kondiah ◽

Lomas K. Tomar ◽

Charu Tyagi ◽

Yahya E. Choonara ◽

Girish Modi ◽

...

Keyword(s):

Multiple Sclerosis ◽

Delivery System ◽

Oral Delivery ◽

Ph Sensitive ◽

Interferon Β ◽

Oral Delivery System

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pH-sensitive polymer-based carriers as a useful approach for oral delivery of therapeutic protein: A review

Protein and Peptide Letters ◽

10.2174/0929866528666210720142841 ◽

2021 ◽

Vol 28 ◽

Author(s):

Maryam Shamseddini lori ◽

Mandana Ohadi ◽

Mohammad Amin Raeisi Estabragh ◽

Sepehr Afsharipour ◽

Ibrahim M Banat ◽

...

Keyword(s):

Spatial Structure ◽

Oral Delivery ◽

Protein A ◽

Protein Structures ◽

Ph Sensitive ◽

Hydrophilic Nature ◽

Stomach Acid ◽

Correct Function ◽

Ph Sensitive Polymer ◽

The Stability

: There are many proteins and enzymes in the human body, and their dysfunction can lead to disease. The use of proteins as a drug is common in various diseases such as diabetes. Proteins are hydrophilic molecules whose spatial structure is critical to their correct function. There are different ways to the administration of proteins. Protein structures are degraded by gastric acid and enzymes in the gastrointestinal tract and have a slight ability to permeation from the gastrointestinal epithelium due to their large hydrophilic nature. Therefore, their oral use has limitations. Since the oral use of drugs is one of the best and easiest routes for patients, many studies have been done to increase the stability, penetration and ultimately increase the bioavailability of proteins through oral administration. One of the studied strategies for oral delivery of protein is the use of pH-sensitive polymer-based carriers. These carriers use different pH-sensitive polymers such as eudragit®, chitosan, dextran, and alginate. The use of pH-sensitive polymer-based carriers by protecting the protein from stomach acid (low pH) and degrading enzymes, increasing permeability, and maintaining the spatial structure of the protein leads to increased bioavailability. In this review, we focus on the various polymers used to prepare pH-sensitive polymer-based carriers for the oral delivery of proteins.

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