Controlled Delivery Formulations

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Physical Pharmacy and Formulation".

Deadline for manuscript submissions: closed (30 November 2020) | Viewed by 50976

Special Issue Editor


E-Mail Website
Guest Editor
Department of Engineering and Pharmaceutical Technology, Faculty of Pharmacy, Miguel Hernandez University, 03550 Alicante, Spain
Interests: dissolutión; controlrelease; disintegration; drug development
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Controlled release formulations are designed to release drug molecules at a specific release rate and at specific sites to maximize therapeutic effects and improve a patient’s compliance.

There are different types of classifications for different controlled release formulations that take into account several factors such as extended release, delayed time, or the strategic release process based on the physiological characteristics in the different administration routes.

Advanced controlled release systems allow for different administrative pathways. Most of these are designed for the oral, parenteral, and transdermal routes, but the controlled release dosage forms of the oral mucosa, the eye, the implantation under the skin, and the nasal route have been developed.

This Special Issue has the aim of highlighting current progress in controlled delivery formulations.

Prof. Dr. Marta González-Álvarez
Guest Editor

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

  • Controlled release
  • Nanoparticles
  • Microparticles
  • Hydrogels
  • Adminsitration routes

Related Special Issue

Published Papers (13 papers)

Order results
Result details
Select all
Export citation of selected articles as:

Editorial

Jump to: Research, Review

3 pages, 179 KiB  
Editorial
Controlled Delivery Formulations
by Marta Gonzalez-Alvarez
Pharmaceutics 2021, 13(3), 374; https://doi.org/10.3390/pharmaceutics13030374 - 12 Mar 2021
Viewed by 1214
Abstract
In the last few decades, controlled release formulations have gained an extraordinary interest [...] Full article
(This article belongs to the Special Issue Controlled Delivery Formulations)

Research

Jump to: Editorial, Review

16 pages, 9813 KiB  
Article
Synthesis and Optimization of Mesoporous Silica Nanoparticles for Ruthenium Polypyridyl Drug Delivery
by Siti Norain Harun, Haslina Ahmad, Hong Ngee Lim, Suet Lin Chia and Martin R. Gill
Pharmaceutics 2021, 13(2), 150; https://doi.org/10.3390/pharmaceutics13020150 - 24 Jan 2021
Cited by 15 | Viewed by 3736
Abstract
The ruthenium polypyridyl complex [Ru(dppz)2PIP]2+ (dppz: dipyridophenazine, PIP: (2-(phenyl)-imidazo[4,5-f ][1,10]phenanthroline), or Ru-PIP, is a potential anticancer drug that acts by inhibiting DNA replication. Due to the poor dissolution of Ru-PIP in aqueous media, a drug delivery agent would be a [...] Read more.
The ruthenium polypyridyl complex [Ru(dppz)2PIP]2+ (dppz: dipyridophenazine, PIP: (2-(phenyl)-imidazo[4,5-f ][1,10]phenanthroline), or Ru-PIP, is a potential anticancer drug that acts by inhibiting DNA replication. Due to the poor dissolution of Ru-PIP in aqueous media, a drug delivery agent would be a useful approach to overcome its limited bioavailability. Mesoporous silica nanoparticles (MSNs) were synthesized via a co-condensation method by using a phenanthrolinium salt with a 16 carbon length chain (Phen-C16) as the template. Optimization of the synthesis conditions by Box–Behnken design (BBD) generated MSNs with high surface area response at 833.9 m2g−1. Ru-PIP was effectively entrapped in MSNs at 18.84%. Drug release profile analysis showed that Ru-PIP is gradually released, with a cumulative release percentage of approximately 50% at 72 h. The release kinetic profile implied that Ru-PIP was released from MSN by diffusion. The in vitro cytotoxicity of Ru-PIP, both free and MSN-encapsulated, was studied in Hela, A549, and T24 cancer cell lines. While treatment of Ru-PIP alone is moderately cytotoxic, encapsulated Ru-PIP exerted significant cytotoxicity upon all the cell lines, with half maximal inhibitory concentration (IC50) values determined by MTT (([3-(4,5-dimethylthiazol-2-yl)-2,5-dephenyltetrazolium bromide]) assay at 48 h exposure substantially decreasing from >30 µM to <10 µM as a result of MSN encapsulation. The mechanistic potential of cytotoxicity on cell cycle distribution showed an increase in G1/S phase populations in all three cell lines. The findings indicate that MSN is an ideal drug delivery agent, as it is able to sustainably release Ru-PIP by diffusion in a prolonged treatment period. Full article
(This article belongs to the Special Issue Controlled Delivery Formulations)
Show Figures

Figure 1

17 pages, 2709 KiB  
Article
pH-Dependent Molecular Gate Mesoporous Microparticles for Biological Control of Giardia intestinalis
by Isabel González-Alvarez, Verónica Vivancos, Carmen Coll, Bárbara Sánchez-Dengra, Elena Aznar, Alejandro Ruiz-Picazo, Marival Bermejo, Félix Sancenón, María Auxiliadora Dea-Ayuela, Marta Gonzalez-Alvarez and Ramón Martínez-Máñez
Pharmaceutics 2021, 13(1), 94; https://doi.org/10.3390/pharmaceutics13010094 - 13 Jan 2021
Cited by 4 | Viewed by 1861
Abstract
Giardiasis is a parasitism produced by the protozoa Giardia intestinalis that lives as trophozoite in the small intestine (mainly in the duodenum) attached to the intestinal villus by means of billed discs. The first line treatment is metronidazole, a drug with high bioavailability, [...] Read more.
Giardiasis is a parasitism produced by the protozoa Giardia intestinalis that lives as trophozoite in the small intestine (mainly in the duodenum) attached to the intestinal villus by means of billed discs. The first line treatment is metronidazole, a drug with high bioavailability, which is why to obtain therapeutic concentrations in duodenum, it is necessary to administer high doses of drug to patients with the consequent occurrence of side effects. It is necessary to developed new therapeutical approaches to achieve a local delivery of the drug. In this sense, we have developed gated mesoporous silica microparticles loaded with metronidazole and with a molecular gate pH dependent. In vitro assays demonstrated that the metronidazole release is practically insignificant at acidic pHs, but in duodenum conditions, the metronidazole delivery from the microparticles is effective enough to produce an important parasite destruction. In vivo assays indicate that this microparticulate system allows to increase the concentration of the drug in duodenum and reduce the concentration in plasma avoiding systemic effects. This system could be useful for other intestinal local treatments in order to reduce doses and increase drug availability in target tissues. Full article
(This article belongs to the Special Issue Controlled Delivery Formulations)
Show Figures

Graphical abstract

19 pages, 2190 KiB  
Article
Aerosolized Niosome Formulation Containing Gemcitabine and Cisplatin for Lung Cancer Treatment: Optimization, Characterization and In Vitro Evaluation
by Norfatin Izzatie Mohamad Saimi, Norazlinaliza Salim, Noraini Ahmad, Emilia Abdulmalek and Mohd Basyaruddin Abdul Rahman
Pharmaceutics 2021, 13(1), 59; https://doi.org/10.3390/pharmaceutics13010059 - 05 Jan 2021
Cited by 36 | Viewed by 3388
Abstract
Gemcitabine (Gem) and cisplatin (Cis) are currently being used for lung cancer treatment, but they are highly toxic in high dosages. This research aimed to develop a niosome formulation containing a low-dosage Gem and Cis (NGC), as an alternative formulation for lung cancer [...] Read more.
Gemcitabine (Gem) and cisplatin (Cis) are currently being used for lung cancer treatment, but they are highly toxic in high dosages. This research aimed to develop a niosome formulation containing a low-dosage Gem and Cis (NGC), as an alternative formulation for lung cancer treatment. NGC was prepared using a very simple heating method and was further optimized by D-optimal mixture design. The optimum NGC formulation with particle size, polydispersity index (PDI), and zeta potential of 166.45 nm, 0.16, and −15.28 mV, respectively, was obtained and remained stable at 27 °C with no phase separation for up to 90 days. The aerosol output was 96.22%, which indicates its suitability as aerosolized formulation. An in vitro drug release study using the dialysis bag diffusion technique showed controlled release for both drugs up to 24 h penetration. A cytotoxicity study against normal lung (MRC5) and lung cancer (A549) cell lines was investigated. The results showed that the optimized NGC had reduced cytotoxicity effects against both MRC5 and A549 when compared with the control (Gem + Cis alone) from very toxic (IC50 < 1.56 µg/mL) to weakly toxic (IC50 280.00 µg/mL) and moderately toxic (IC50 = 46.00 µg/mL), respectively, after 72 h of treatment. These findings revealed that the optimized NGC has excellent potential and is a promising prospect in aerosolized delivery systems to treat lung cancer that warrants further investigation. Full article
(This article belongs to the Special Issue Controlled Delivery Formulations)
Show Figures

Figure 1

14 pages, 3120 KiB  
Article
Antibacterial Activity of Linezolid against Gram-Negative Bacteria: Utilization of ε-Poly-l-Lysine Capped Silica Xerogel as an Activating Carrier
by Gulcihan Guzel Kaya, Serena Medaglia, Vicente Candela-Noguera, María Ángeles Tormo-Mas, María Dolores Marcos, Elena Aznar, Huseyin Deveci and Ramón Martínez-Máñez
Pharmaceutics 2020, 12(11), 1126; https://doi.org/10.3390/pharmaceutics12111126 - 21 Nov 2020
Cited by 12 | Viewed by 2886
Abstract
In recent times, many approaches have been developed against drug resistant Gram-negative bacteria. However, low-cost high effective materials which could broaden the spectrum of antibiotics are still needed. In this study, enhancement of linezolid spectrum, normally active against Gram-positive bacteria, was aimed for [...] Read more.
In recent times, many approaches have been developed against drug resistant Gram-negative bacteria. However, low-cost high effective materials which could broaden the spectrum of antibiotics are still needed. In this study, enhancement of linezolid spectrum, normally active against Gram-positive bacteria, was aimed for Gram-negative bacteria growth inhibition. For this purpose, a silica xerogel prepared from a low-cost precursor is used as a drug carrier owing to the advantages of its mesoporous structure, suitable pore and particle size and ultralow density. The silica xerogel is loaded with linezolid and capped with ε-poly-l-lysine. The developed nano-formulation shows a marked antibacterial activity against to Escherichia coli, Pseudomonas aeruginosa and Staphylococcus aureus. In comparison to free linezolid and ε-poly-l-lysine, the material demonstrates a synergistic effect on killing for the three tested bacteria. The results show that silica xerogels can be used as a potential drug carrier and activity enhancer. This strategy could provide the improvement of antibacterial activity spectrum of antibacterial agents like linezolid and could represent a powerful alternative to overcome antibiotic resistance in a near future. Full article
(This article belongs to the Special Issue Controlled Delivery Formulations)
Show Figures

Graphical abstract

17 pages, 2925 KiB  
Article
Performance and Stability of Tenofovir Alafenamide Formulations within Subcutaneous Biodegradable Implants for HIV Pre-Exposure Prophylaxis (PrEP)
by Linying Li, Leah M. Johnson, Sai Archana Krovi, Zach R. Demkovich and Ariane van der Straten
Pharmaceutics 2020, 12(11), 1057; https://doi.org/10.3390/pharmaceutics12111057 - 05 Nov 2020
Cited by 19 | Viewed by 3803
Abstract
A critical need exists to develop diverse biomedical strategies for the widespread use of HIV Pre-Exposure Prophylaxis (HIV PrEP). This manuscript describes a subcutaneous reservoir-style implant for long-acting delivery of tenofovir alafenamide (TAF) for HIV PrEP. We detail key parameters of the TAF [...] Read more.
A critical need exists to develop diverse biomedical strategies for the widespread use of HIV Pre-Exposure Prophylaxis (HIV PrEP). This manuscript describes a subcutaneous reservoir-style implant for long-acting delivery of tenofovir alafenamide (TAF) for HIV PrEP. We detail key parameters of the TAF formulation that affect implant performance, including TAF ionization form, the selection of excipient and the exposure to aqueous conditions. Both in-vitro studies and shelf stability tests demonstrate enhanced performance for TAF freebase (TAFFB) in this long-acting implant platform, as TAFFB maintains higher chemical stability than the TAF hemifumarate salt (TAFHF). We also examined the hydrolytic degradation profiles of various formulations of TAF and identified inflection points for the onset of the accelerated drug hydrolysis within the implant using a two-line model. The compositions of unstable formulations are characterized by liquid chromatography-mass spectrometry (LC-MS) and are correlated to predominant products of the TAF hydrolytic pathways. The hydrolysis rate of TAF is affected by pH and water content in the implant microenvironment. We further demonstrate the ability to substantially delay the degradation of TAF by reducing the rates of drug release and thus lowering the water ingress rate. Using this approach, we achieved sustained release of TAFFB formulations over 240 days and maintained > 93% TAF purity under simulated physiological conditions. The opportunities for optimization of TAF formulations in this biodegradable implant supports further advancement of strategies to address long-acting HIV PrEP. Full article
(This article belongs to the Special Issue Controlled Delivery Formulations)
Show Figures

Figure 1

13 pages, 2141 KiB  
Article
Ex-Vivo Trans-Corneal and Trans-Scleral Diffusion Studies with Ocular Formulations of Glutathione as an Antioxidant Treatment for Ocular Diseases
by María Sebastián-Morelló, Adrián M. Alambiaga-Caravaca, María Aracely Calatayud-Pascual, Vicent Rodilla, Cristina Balaguer-Fernández, María Miranda and Alicia López-Castellano
Pharmaceutics 2020, 12(9), 861; https://doi.org/10.3390/pharmaceutics12090861 - 10 Sep 2020
Cited by 6 | Viewed by 3746
Abstract
Exposure to sunlight and contact with atmospheric oxygen makes the eye particularly susceptible to oxidative stress, which can potentially produce cellular damage. In physiological conditions, there are several antioxidant defense mechanisms within the eye. Glutathione (GSH) is the most important antioxidant in the [...] Read more.
Exposure to sunlight and contact with atmospheric oxygen makes the eye particularly susceptible to oxidative stress, which can potentially produce cellular damage. In physiological conditions, there are several antioxidant defense mechanisms within the eye. Glutathione (GSH) is the most important antioxidant in the eye; GSH deficit has been linked to several ocular pathologies. The aim of this study was to explore the potential for newly developed formulations allowing controlled delivery of antioxidants such as GSH and vitamin C (Vit C) directly to the eye. We have investigated the stability of antioxidants in aqueous solution and assessed ex-vivo the diffusion of GSH through two ocular membranes, namely cornea and sclera, either in solution or included in a semisolid insert. We have also carried out the hen’s egg-chlorioallantoic membrane test (HET-CAM) to evaluate the ocular irritancy of the different antioxidant solutions. Our results showed that GSH is stable for up to 30 days at 4 °C in darkness and it is not an irritant to the eye. The diffusion studies revealed that the manufactured formulation, a semisolid insert containing GSH, could deliver this tripeptide directly to the eye in a sustained manner. Full article
(This article belongs to the Special Issue Controlled Delivery Formulations)
Show Figures

Graphical abstract

18 pages, 6667 KiB  
Article
Nicardipine Loaded Solid Phospholipid Extrudates for the Prevention of Cerebral Vasospasms: In Vitro Characterization
by Christin Zlomke, Johannes Albrecht and Karsten Mäder
Pharmaceutics 2020, 12(9), 817; https://doi.org/10.3390/pharmaceutics12090817 - 28 Aug 2020
Cited by 4 | Viewed by 2636
Abstract
The aim of the study was to develop nicardipine loaded phospholipid extrudates as an alternative for PLA/PLGA-based implants for the prevention of cerebral vasospasms. Extrudates of different mixtures of saturated and unsaturated phosphatidylcholine (PC) were produced and characterized by DSC, microscopy and texture [...] Read more.
The aim of the study was to develop nicardipine loaded phospholipid extrudates as an alternative for PLA/PLGA-based implants for the prevention of cerebral vasospasms. Extrudates of different mixtures of saturated and unsaturated phosphatidylcholine (PC) were produced and characterized by DSC, microscopy and texture analysis. Single phospholipid components were identified by ELSD-HPLC. Extrudates of 2 mm diameter were obtained by twin screw extrusion temperatures below 50 °C. The ratio of unsaturated and saturated phosphatidylcholine components determines the physicochemical properties of the extrudates as well as the rate of erosion. Nicardipine loaded phospholipids extrudates released the drug over several weeks in vitro. The phospholipid composition of the remaining extrudate changed during the release, the content of unsaturated phospholipids decreased faster compared to the saturated ones. In conclusion, solid phospholipid extrudates are promising materials for the development of new parenteral controlled release systems. Full article
(This article belongs to the Special Issue Controlled Delivery Formulations)
Show Figures

Graphical abstract

21 pages, 6173 KiB  
Article
Controlled Release of Doxorubicin from the Drug Delivery Formulation Composed of Single-Walled Carbon Nanotubes and Congo Red: A Molecular Dynamics Study and Dynamic Light Scattering Analysis
by Anna Jagusiak, Katarzyna Chlopas, Grzegorz Zemanek, Pawel Wolski and Tomasz Panczyk
Pharmaceutics 2020, 12(7), 622; https://doi.org/10.3390/pharmaceutics12070622 - 03 Jul 2020
Cited by 13 | Viewed by 2648
Abstract
The controlled delivery and release of drug molecules at specific targets increases the therapeutic efficacy of treatment. This paper presents a triple complex which is a new potential drug delivery system. Triple complex contains single-walled carbon nanotubes, Congo red, and doxorubicin. Nanotubes are [...] Read more.
The controlled delivery and release of drug molecules at specific targets increases the therapeutic efficacy of treatment. This paper presents a triple complex which is a new potential drug delivery system. Triple complex contains single-walled carbon nanotubes, Congo red, and doxorubicin. Nanotubes are built of a folded graphene layer providing a large surface for binding Congo red via “face-to-face” stacking which markedly increases the binding capacity of the carrier. Congo red is a compound that self-associates to form supramolecular ribbon-like structures, which are able to bind some drugs by intercalation. The nanotube–Congo red complex can bind the model drug doxorubicin. Thus, a new triple carrier system was obtained. The aim of this paper is to present studies on the controlled release of a model anticancer drug from a triple carrier system through pH changes. The specific aim of the study was to model the structure of the obtained experimental systems and to compare the changes in the average energy of interaction between its components induced by pH changes. The studies also aimed to compare the intensity of pH-dependent changes in hydrodynamic diameters of individual components of the triple carrier system. The effect of pH changes on the stability of the analyzed systems was examined using the molecular modeling method and dynamic light scattering. The decrease in pH influenced the structure and stability of the analyzed triple systems and ensured efficient drug release. The changes in hydrodynamic diameters of the obtained fractions were examined with the use of dynamic light scattering and were confirmed by computer simulation methods. The formulation presented in this paper shows potential for a therapeutic application owing to its high drug binding capacity and pH-dependent release. This ensures prolonged local action of the drug. The results reveal that the studied complex fulfills the basic requirements for its potential use as drug carrier, thus reducing side effects and enhancing pharmacological efficacy of drugs. Full article
(This article belongs to the Special Issue Controlled Delivery Formulations)
Show Figures

Graphical abstract

17 pages, 7378 KiB  
Article
The Correlation between Physical Crosslinking and Water-Soluble Drug Release from Chitosan-Based Microparticles
by Emilia Szymańska, Katarzyna Woś-Latosi, Julia Jacyna, Magdalena Dąbrowska, Joanna Potaś, Michał Jan Markuszewski and Katarzyna Winnicka
Pharmaceutics 2020, 12(5), 455; https://doi.org/10.3390/pharmaceutics12050455 - 16 May 2020
Cited by 5 | Viewed by 2557
Abstract
Microparticles containing water-soluble zidovudine were prepared by spray-drying using chitosan glutamate and beta-glycerophosphate as an ion crosslinker (CF). The Box–Behnken design was applied to optimize the microparticles in terms of their drug loading and release behavior. Physicochemical studies were undertaken to support the [...] Read more.
Microparticles containing water-soluble zidovudine were prepared by spray-drying using chitosan glutamate and beta-glycerophosphate as an ion crosslinker (CF). The Box–Behnken design was applied to optimize the microparticles in terms of their drug loading and release behavior. Physicochemical studies were undertaken to support the results from dissolution tests and to evaluate the impact of the crosslinking ratio on the microparticles’ characteristics. The zidovudine dissolution behavior had a complex nature which comprised two phases: an initial burst effect followed with a prolonged release stage. The initial drug release, which can be modulated by the crosslinking degree, was primarily governed by the dissolution of the drug crystals located on the microparticles’ surfaces. In turn, the further dissolution stage was related to the drug diffusion from the swollen polymer matrix and was found to correlate with the drug loading. Differential Scanning Calorimetry (DSC) studies revealed the partial incorporation of a non-crystallized drug within the polymer matrix, which correlated with the amount of CF. Although CF influenced the swelling capacity of chitosan glutamate microparticles, surprisingly a higher amount of CF did not impact the time required for 80% of the drug to be released markedly. The formulation with the lowest polymer:CF ratio, 3:1, was selected as optimal, providing satisfactory drug loading and displaying a moderate burst effect within the first 30 min of the study, followed with a prolonged drug release of up to 210 min. Full article
(This article belongs to the Special Issue Controlled Delivery Formulations)
Show Figures

Graphical abstract

14 pages, 1856 KiB  
Article
In Vitro Evaluation of Antimicrobial Activity of Minocycline Formulations for Topical Application in Periodontal Therapy
by Jan-Luca Schmid, Martin Kirchberg, Sandra Sarembe, Andreas Kiesow, Anton Sculean, Karsten Mäder, Mirko Buchholz and Sigrun Eick
Pharmaceutics 2020, 12(4), 352; https://doi.org/10.3390/pharmaceutics12040352 - 13 Apr 2020
Cited by 16 | Viewed by 3311
Abstract
Periodontal therapy using antimicrobials that are topically applied requires slow or controlled release devices. The in vitro antimicrobial activity of biodegradable polymer formulations that contain a new minocycline lipid complex (P-MLC) was evaluated. The new P-MLC formulations that contained 11.5% minocycline were compared [...] Read more.
Periodontal therapy using antimicrobials that are topically applied requires slow or controlled release devices. The in vitro antimicrobial activity of biodegradable polymer formulations that contain a new minocycline lipid complex (P-MLC) was evaluated. The new P-MLC formulations that contained 11.5% minocycline were compared with pure minocycline or an existing commercial formulation, which included determination of minimal inhibitory concentration (MIC) values against two oral bacteria and activity on six-species periodontal biofilm. Moreover, the flow of gingival crevicular fluid (GCF) was modeled up to 42 days and the obtained eluates were tested both for MIC values and inhibiting biofilm formation. In general, MICs of the P-MLC formulations were slightly increased as compared with pure minocycline. Biofilm formation was clearly inhibited by all tested formulations containing minocycline with no clear difference between them. In 3.5 day old biofilms, all formulations with 250 µg/mL minocycline decreased bacterial counts by 3 log10 and metabolic activity with no difference to pure antimicrobials. Eluates of experimental formulations showed superiority in antimicrobial activity. Eluates of one experimental formulation (P503-MLC) still inhibited biofilm formation at 28 days, with a reduction by 1.87 log10 colony forming units (CFU) vs. the untreated control. The new experimental formulations can easily be instilled in periodontal pockets and represent alternatives in local antimicrobials, and thus warrant further testing. Full article
(This article belongs to the Special Issue Controlled Delivery Formulations)
Show Figures

Figure 1

Review

Jump to: Editorial, Research

33 pages, 1943 KiB  
Review
Progress in Mesoporous Silica Nanoparticles as Drug Delivery Agents for Cancer Treatment
by Eleen Dayana Mohamed Isa, Haslina Ahmad, Mohd Basyaruddin Abdul Rahman and Martin R. Gill
Pharmaceutics 2021, 13(2), 152; https://doi.org/10.3390/pharmaceutics13020152 - 24 Jan 2021
Cited by 57 | Viewed by 6895
Abstract
Cancer treatment and therapy have made significant leaps and bounds in these past decades. However, there are still cases where surgical removal is impossible, metastases are challenging, and chemotherapy and radiotherapy pose severe side effects. Therefore, a need to find more effective and [...] Read more.
Cancer treatment and therapy have made significant leaps and bounds in these past decades. However, there are still cases where surgical removal is impossible, metastases are challenging, and chemotherapy and radiotherapy pose severe side effects. Therefore, a need to find more effective and specific treatments still exists. One way is through the utilization of drug delivery agents (DDA) based on nanomaterials. In 2001, mesoporous silica nanoparticles (MSNs) were first used as DDA and have gained considerable attention in this field. The popularity of MSNs is due to their unique properties such as tunable particle and pore size, high surface area and pore volume, easy functionalization and surface modification, high stability and their capability to efficiently entrap cargo molecules. This review describes the latest advancement of MSNs as DDA for cancer treatment. We focus on the fabrication of MSNs, the challenges in DDA development and how MSNs address the problems through the development of smart DDA using MSNs. Besides that, MSNs have also been applied as a multifunctional DDA where they can serve in both the diagnostic and treatment of cancer. Overall, we argue MSNs provide a bright future for both the diagnosis and treatment of cancer. Full article
(This article belongs to the Special Issue Controlled Delivery Formulations)
Show Figures

Figure 1

63 pages, 3306 KiB  
Review
Polymer Selection for Hot-Melt Extrusion Coupled to Fused Deposition Modelling in Pharmaceutics
by Gabriela G. Pereira, Sara Figueiredo, Ana Isabel Fernandes and João F. Pinto
Pharmaceutics 2020, 12(9), 795; https://doi.org/10.3390/pharmaceutics12090795 - 22 Aug 2020
Cited by 64 | Viewed by 11512
Abstract
Three-dimensional (3D) printing offers the greatest potential to revolutionize the future of pharmaceutical manufacturing by overcoming challenges of conventional pharmaceutical operations and focusing design and production of dosage forms on the patient’s needs. Of the many technologies available, fusion deposition modelling (FDM) is [...] Read more.
Three-dimensional (3D) printing offers the greatest potential to revolutionize the future of pharmaceutical manufacturing by overcoming challenges of conventional pharmaceutical operations and focusing design and production of dosage forms on the patient’s needs. Of the many technologies available, fusion deposition modelling (FDM) is considered of the lowest cost and higher reproducibility and accessibility, offering clear advantages in drug delivery. FDM requires in-house production of filaments of drug-containing thermoplastic polymers by hot-melt extrusion (HME), and the prospect of connecting the two technologies has been under investigation. The ability to integrate HME and FDM and predict and tailor the filaments’ properties will extend the range of printable polymers/formulations. Hence, this work revises the properties of the most common pharmaceutical-grade polymers used and their effect on extrudability, printability, and printing outcome, providing suitable processing windows for different raw materials. As a result, formulation selection will be more straightforward (considering the characteristics of drug and desired dosage form or release profile) and the processes setup will be more expedite (avoiding or mitigating typical processing issues), thus guaranteeing the success of both HME and FDM. Relevant techniques used to characterize filaments and 3D-printed dosage forms as an essential component for the evaluation of the quality output are also presented. Full article
(This article belongs to the Special Issue Controlled Delivery Formulations)
Show Figures

Graphical abstract

Back to TopTop