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Pharmaceutics
Special Issues
Lymphatic Aspects of Drug Delivery, Formulation, and Bioavailability
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Lymphatic Aspects of Drug Delivery, Formulation, and Bioavailability

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Delivery and Controlled Release".

Deadline for manuscript submissions: closed (31 December 2024) | Viewed by 2354

Special Issue Editors

Prof. Dr. Neal M. Davies

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Guest Editor
Faculty of Pharmacy and Pharmaceutical Sciences, Katz Group-Rexall Centre for Pharmacy & Health Research, University of Alberta, 11315–87 Avenue, Edmonton, AB T6G 2E1, Canada
Interests: pharmacokinetics; chirality; drug interactions; formulation and drug delivery
Special Issues, Collections and Topics in MDPI journals
Dr. Nadia Araci Bou-Chacra

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Guest Editor
Faculty of Pharmaceutical Sciences, University of Sao Paulo, Sao Paulo 05508-000, Brazil
Interests: drug nanocrystals; lipid nanoparticles; quality by design; ophthalmic drug delivery
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Raimar Löbenberg

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Guest Editor
Faculty of Pharmacy & Pharmaceutical Sciences, Katz Group-Rexall Centre for Pharmacy & Health Research, University of Alberta, 11361–87 Avenue, Edmonton, AB T6G 2E1, Canada
Interests: biopharmaceutics; inhalable nanopartilces; traditional medicines
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The lymphatic system plays a pivotal role in immune response and fluid balance and offers a promising alternative pathway for targeted drug delivery and disposition. Pharmaceutical advancements in lymphatic delivery and disposition encompass a spectrum of techniques and formulations aimed at optimizing bioavailability, stability, and therapeutic efficacy of drugs.

This Special Issue will delve into diverse facets of lymphatic delivery and disposition, spanning traditional, contemporary, and cutting-edge methodologies. From exploring novel carriers for enhanced bioavailability to unravelling the intricacies of dissolution, lipolysis, release kinetics, and stability concerns, this Special Issue will elucidate strategies to harness the lymphatic system for improved therapeutic outcomes.

Key topics to be addressed include the following:

  • Targeted Delivery Systems: investigating innovative delivery systems tailored to exploit the lymphatic route for precise drug targeting and modified release;
  • Bioavailability Enhancement: formulation techniques and strategies to enhance the bioavailability of drugs through lymphatic absorption, overcoming barriers such as poor solubility and permeability;
  • Release Kinetics and Stability: analyzing the kinetics of drug release within the lymphatic system and addressing stability challenges to ensure optimal therapeutic efficacy;
  • Toxicity and Safety: assessing the impact of lymphatic delivery on drug toxicity and safety profiles, with a focus on mitigating adverse effects and improving patient outcomes;
  • Innovative Technologies and Clinical Applications: exploring emerging technologies and methodologies, including nanomedicine and lipid-based formulations, lymphatic dissolution techniques, PBPK models, and targeted lymphatic drug delivery and disposition.

By fostering interdisciplinary pharmaceutical discourse and sharing cutting-edge research, this Special Issue aims to advance our understanding of lymphatic delivery and disposition, paving the way for the development of novel therapeutic interventions with enhanced efficacy and safety profiles.

We invite contributions spanning original research articles, reviews, and perspectives that shed light on the pharmaceutical aspects of lymphatic delivery and disposition, driving innovation and transformation in drug development and delivery.

We look forward to your valuable insights and contributions.

Prof. Dr. Neal M. Davies
Prof. Dr. Nadia Araci Bou-Chacra
Prof. Dr. Raimar Löbenberg
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceutics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • targeted delivery systems
  • bioavailability enhancement
  • release kinetics
  • dissolution, solubility, and stability
  • toxicity and safety
  • lipid-based formulations and lipolysis

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Published Papers (2 papers)

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13 pages, 2069 KiB  
Article
In Vitro Predictive Model for Intestinal Lymphatic Uptake: Exploration of Additional Enhancers and Inhibitors
by Malaz Yousef, Conor O’Croinin, Tyson S. Le, Chulhun Park, Jieyu Zuo, Nadia Bou Chacra, Neal M. Davies and Raimar Löbenberg
Pharmaceutics 2024, 16(6), 768; https://doi.org/10.3390/pharmaceutics16060768 - 5 Jun 2024
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Abstract
Drug absorption via chylomicrons holds significant implications for both pharmacokinetics and pharmacodynamics. However, a mechanistic understanding of predicting in vivo intestinal lymphatic uptake remains largely unexplored. This study aimed to delve into the intestinal lymphatic uptake of drugs, investigating both enhancement and inhibition [...] Read more.
Drug absorption via chylomicrons holds significant implications for both pharmacokinetics and pharmacodynamics. However, a mechanistic understanding of predicting in vivo intestinal lymphatic uptake remains largely unexplored. This study aimed to delve into the intestinal lymphatic uptake of drugs, investigating both enhancement and inhibition using various excipients through our previously established in vitro model. It also examined the applicability of the model by assessing the lymphatic uptake enhancement of a lymphotropic formulation with linoleoyl polyoxyl-6 glycerides using the same model. The model successfully differentiated among olive, sesame, and peanut oils in terms of lymphatic uptake. However, it did not distinguish between oils containing long-chain fatty acids and coconut oil. Coconut oil, known for its abundance of medium-chain fatty acids, outperformed other oils. This heightened uptake was attributed to the superior emulsification of this oil in artificial chylomicron media due to its high content of medium-chain fatty acids. Additionally, the enhanced uptake of the tested formulation with linoleoyl polyoxyl-6 glycerides underscored the practical applicability of this model in formulation optimization. Moreover, data suggested that increasing the zeta potential of Intralipid® using sodium lauryl sulfate (SLS) and decreasing it using (+/−) chloroquine led to enhanced and reduced uptake in the in vitro model, respectively. These findings indicate the potential influence of the zeta potential on intestinal lymphatic uptake in this model, though further research is needed to explore the possible translation of this mechanism in vivo. Full article
(This article belongs to the Special Issue Lymphatic Aspects of Drug Delivery, Formulation, and Bioavailability)
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27 pages, 3326 KiB  
Systematic Review
Emerging Pharmacological Interventions for Chronic Venous Insufficiency: A Comprehensive Systematic Review and Meta-Analysis of Efficacy, Safety, and Therapeutic Advances
by Camila Botelho Miguel, Ranielly de Souza Andrade, Laise Mazurek, Melissa Carvalho Martins-de-Abreu, Jamil Miguel-Neto, Aurélio de Melo Barbosa, Glicélia Pereira Silva, Aristóteles Góes-Neto, Siomar de Castro Soares, Javier Emilio Lazo-Chica and Wellington Francisco Rodrigues
Pharmaceutics 2025, 17(1), 59; https://doi.org/10.3390/pharmaceutics17010059 - 3 Jan 2025
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Abstract
Background/Objectives: Chronic Venous Insufficiency (CVI) is a progressive vascular condition characterized by venous hypertension and chronic inflammation, leading to significant clinical and socioeconomic impacts. This study aimed to evaluate the efficacy and safety of emerging pharmacological interventions for CVI, focusing on clinical outcomes [...] Read more.
Background/Objectives: Chronic Venous Insufficiency (CVI) is a progressive vascular condition characterized by venous hypertension and chronic inflammation, leading to significant clinical and socioeconomic impacts. This study aimed to evaluate the efficacy and safety of emerging pharmacological interventions for CVI, focusing on clinical outcomes such as pain, edema, cutaneous blood flow, and quality of life. Methods: Eligible interventions comprised new vasoprotective drugs, such as hydroxyethylrutoside, Pycnogenol, aminaphthone, coumarin + troxerutin, and Venoruton, compared to the standard therapy of diosmin and hesperidin. Results: Hydroxyethylrutoside and Pycnogenol showed significant benefits in pain reduction and resting flux improvement, with mean differences of 38 (95% CI: 10.56–65.44) and 25.30 (95% CI: 18.73–31.87), respectively. Improvements in edema and quality of life were less consistent. Substantial heterogeneity was observed (I2 = 100%, p < 0.001). Conclusions: Hydroxyethylrutoside and Pycnogenol emerge as promising alternatives for managing CVI. However, limitations such as high heterogeneity, small sample sizes, and methodological inconsistencies highlight the need for more robust and standardized clinical trials. This study underscores the importance of personalized and cost-effective strategies, particularly in resource-limited settings. Full article
(This article belongs to the Special Issue Lymphatic Aspects of Drug Delivery, Formulation, and Bioavailability)
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