Improved Bioavailability of Poorly Soluble Drugs through Gastrointestinal Muco-Adhesion of Lipid Nanoparticles

Tan, Sui Ling Janet; Billa, Nashiru

doi:10.3390/pharmaceutics13111817

Cited by 30 publications

(16 citation statements)

References 167 publications

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“…Industrially, chemical treatment for acid degradation is preferred because it is convenient, low-cost, fast, scalable, and produces reproducible CS–LMW mixtures [ 52 , 53 ]. The use of NaNO 2 showed the best performance for CS degradation [ 39 ]. Variations in the amount of NaNO 2 and reaction time obtained two samples of CS with Mw 20 kDa ( Table 2 ).…”

Section: Resultsmentioning

confidence: 99%

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Cytotoxicity Enhancement in MCF-7 Breast Cancer Cells with Depolymerized Chitosan Delivery of α-Mangostin

et al. 2022

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The application of α-mangostin (AMG) in breast cancer research has wide intentions. Chitosan-based nanoparticles (CSNPs) have attractive prospects for developing anticancer drugs, especially in their high flexibility for modification to enhance their anticancer action. This research aimed to study the impact of depolymerized chitosan (CS) on the cytotoxicity enhancement of AMG in MCF-7 breast cancer cells. CSNPs effectivity depends on size, shape, crystallinity degree, and charge surface. Modifying CS molecular weight (MW) is expected to influence CSNPs’ characteristics, impacting size, shape, crystallinity degree, and charge surface. CSNPs are developed using the method of ionic gelation with sodium tripolyphosphate (TPP) as a crosslinker and spray pyrolysis procedure. Nanoparticles’ (NPs) sizes vary from 205.3 ± 81 nm to 450.9 ± 235 nm, ZP charges range from +10.56 mV to +51.56 mV, and entrapment efficiency from 85.35% to 90.45%. The morphology of NPs are all the same spherical forms. In vitro release studies confirmed that AMG–Chitosan–High Molecular Weight (AMG–CS–HMW) and AMG–Chitosan–Low Molecular Weight (AMG–CS–LMW) had a sustained-release system profile. MW has a great influence on surface, drug release, and cytotoxicity enhancement of AMG in CSNPs to MCF-7 cancer cells. The preparations AMG–CS–HMW and AMG–CS–LMW NPs considerably enhanced the cytotoxicity of MCF-7 cells with IC50 values of 5.90 ± 0.08 µg/mL and 4.90 ± 0.16 µg/mL, respectively, as compared with the non-nano particle formulation with an IC50 of 8.47 ± 0.29 µg/mL. These findings suggest that CSNPs can enhance the physicochemical characteristics and cytotoxicity of AMG in breast cancer treatment.

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Section: Resultsmentioning

confidence: 99%

“…TPP was dissolved in distilled water at various concentrations, filtered through a syringe filter (0.22 µm), and chilled to 2–4 °C in another beaker. Finally, five milliliters of TPP solution were added to ten milliliters of CS solution and mixed for ten minutes [ 39 ]. Spray pyrolysis equipment was used to obtain NPs [ 40 ].…”

Section: Methodsmentioning

confidence: 99%

Cytotoxicity Enhancement in MCF-7 Breast Cancer Cells with Depolymerized Chitosan Delivery of α-Mangostin

et al. 2022

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“…For at least the past four decades, multiple research groups have searched for materials for the development of mucoadhesive and/or mucopenetrating pharmaceutical formulations to improve the bioavailability of active constituents [ 101 , 102 , 103 , 104 ]. Both the adhesive and mucopenetrating properties of particulate adjuvants allow them to reach the epithelial barrier.…”

Section: Mucoadhesive and Mucopenetrating Polymer-based Adjuvantsmentioning

confidence: 99%

The Role of Mucoadhesion and Mucopenetration in the Immune Response Induced by Polymer-Based Mucosal Adjuvants

et al. 2023

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Mucus is a viscoelastic gel that acts as a protective barrier for epithelial surfaces. The mucosal vehicles and adjuvants need to pass through the mucus layer to make drugs and vaccine delivery by mucosal routes possible. The mucoadhesion of polymer particle adjuvants significantly increases the contact time between vaccine formulations and the mucosa; then, the particles can penetrate the mucus layer and epithelium to reach mucosa-associated lymphoid tissues. This review presents the key findings that have aided in understanding mucoadhesion and mucopenetration while exploring the influence of physicochemical characteristics on mucus–polymer interactions. We describe polymer-based particles designed with mucoadhesive or mucopenetrating properties and discuss the impact of mucoadhesive polymers on local and systemic immune responses after mucosal immunization. In future research, more attention paid to the design and development of mucosal adjuvants could lead to more effective vaccines.

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“…SLNs and NLCs are alternatives to micelles, emulsions, liposomes, and polymeric nanoparticles in drug delivery. They have some distinct advantages that facilitate their wider applications for oral, parenteral, intranasal, ocular, transdermal, and pulmonary drug delivery [ 44 , 45 , 46 ]. The components of SLNs and NLCs are physiologically biocompatible and biodegradable lipids and other excipients that are generally recognized as safe (GRAS), making them safe nano-drug delivery systems [ 47 , 48 ].…”

Section: Nose-to-brain Delivery Pathways and Feasibilities Of Slns An...mentioning

confidence: 99%

Pharmacokinetics and Pharmacodynamics of Intranasal Solid Lipid Nanoparticles and Nanostructured Lipid Carriers for Nose-to-Brain Delivery

Nguyen

Maeng

2022

Pharmaceutics

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Nose-to-brain drug delivery has been of great interest for the treatment of many central nervous system (CNS) diseases and psychiatric disorders over past decades. Several nasally administered formulations have been developed to circumvent the blood-brain barrier and directly deliver drugs to the CNS through the olfactory and trigeminal pathways. However, the nasal mucosa’s drug absorption is insufficient and the volume of the nasal cavity is small, which, in combination, make nose-to-brain drug delivery challenging. These problems could be minimized using formulations based on solid lipid nanoparticles (SLNs) or nanostructured lipid carriers (NLCs), which are effective nose-to-brain drug delivery systems that improve drug bioavailability by increasing drug solubility and permeation, extending drug action, and reducing enzymatic degradation. Various research groups have reported in vivo pharmacokinetics and pharmacodynamics of SLNs and NLCs nose-to-brain delivery systems. This review was undertaken to provide an overview of these studies and highlight research performed on SLN and NLC-based formulations aimed at improving the treatment of CNS diseases such neurodegenerative diseases, epilepsy, and schizophrenia. We discuss the efficacies and brain targeting efficiencies of these formulations based on considerations of their pharmacokinetic parameters and toxicities, point out some gaps in current knowledge, and propose future developmental targets.

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Improved Bioavailability of Poorly Soluble Drugs through Gastrointestinal Muco-Adhesion of Lipid Nanoparticles

Cited by 30 publications

References 167 publications

Cytotoxicity Enhancement in MCF-7 Breast Cancer Cells with Depolymerized Chitosan Delivery of α-Mangostin

Cytotoxicity Enhancement in MCF-7 Breast Cancer Cells with Depolymerized Chitosan Delivery of α-Mangostin

The Role of Mucoadhesion and Mucopenetration in the Immune Response Induced by Polymer-Based Mucosal Adjuvants

Pharmacokinetics and Pharmacodynamics of Intranasal Solid Lipid Nanoparticles and Nanostructured Lipid Carriers for Nose-to-Brain Delivery

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