Insights into Biodegradable Polymer-Based Delivery Vehicles for Pharmaceutical Applications: Traditional and Current Approaches

A special issue of Polymers (ISSN 2073-4360). This special issue belongs to the section "Smart and Functional Polymers".

Deadline for manuscript submissions: closed (25 July 2023) | Viewed by 10672

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Guest Editor
Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt
Interests: drug delivery; polymeric delivery systems; nanoplatforms; sustained drug release; scaffolds; implants; tissue engineering; wound healing; brain targeting; pulmonary delivery; cancer
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Special Issue Information

Dear Colleagues,

Biodegradable polymers, either natural or synthetic, represent a distinctive class of polymers widely used for delivering active moieties (drugs, DNA, RNA, etc.). Biocompatibility offers the magic possible option for different delivery systems. Natural polymers, such as alginate, zein, and hyaluronates, besides synthetic ones, such as polylactic acid, poly(lactic-co-glycolic) acid, and polycaprolactone, are broadly used for the fabrication of different nanoplatforms, microparticles, hydrogels, scaffolds, and implants which aim to enhance the targeting, delivery, and bioavailability of active moieties, with the exception of boosting tissue regeneration. Combining different types of polymers or adding chemical functionalities to them can present a new paradigm for novel advances in delivery of therapeutics. Using smart biodegradable polymers, including chitosan, paves the way for the fabrication of delivery systems which can modify their characteristics as a response to external stimuli such as pH, light, temperature, and electric or magnetic fields. Moreover, enhancing the outcomes of using biodegradable polymers in the pharmaceutical field can be obtained by applying different fabrication strategies, e.g., the inclusion of stem cells, which will differentiate into different cells, as well as the formation of suitable inks or bioinks for 3D and 4D printing required for the success of different microfluidic systems.

This Special Issue invites researchers to submit original research and review articles which highlight traditional and current updates of using biodegradable polymers in the pharmaceutical field.

Dr. Nermeen Adel Elkasabgy
Guest Editor

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Keywords

  • biodegradable polymers
  • peptides
  • drugs
  • DNA
  • enhanced bioavailability
  • tissue regeneration
  • nanoplatforms
  • microparticles
  • scaffolds
  • hydrogels

Published Papers (5 papers)

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Research

17 pages, 2211 KiB  
Article
Ceftriaxone-Loaded Polymeric Microneedles, Dressings, and Microfibers for Wound Treatment
by Pablo Serrano-Castañeda, Miguel Alejandro Ochoa Loyo, Cristian Ezequiel Tinoco Hernández, Brian Miguel Anaya-Ortega, Omar Rodrigo Guadarrama-Escobar, Ericka Anguiano-Almazán, Betsabé Rodríguez-Pérez, Ma. Concepción Peña-Juárez, Alma Vázquez-Durán, Abraham Méndez-Albores, Isabel Marlen Rodríguez-Cruz, Miriam Isabel Morales-Florido and José Juan Escobar-Chávez
Polymers 2023, 15(12), 2610; https://0-doi-org.brum.beds.ac.uk/10.3390/polym15122610 - 8 Jun 2023
Viewed by 1419
Abstract
The objective of this study was to create polymeric dressings, microfibers, and microneedles (MN) loaded with ceftriaxone, using PMVA (Poly (Methyl vinyl ether-alt-maleic acid), Kollicoat® 100P, and Kollicoat® Protect as polymers to treat diabetic wounds and accelerate their recovery. These formulations [...] Read more.
The objective of this study was to create polymeric dressings, microfibers, and microneedles (MN) loaded with ceftriaxone, using PMVA (Poly (Methyl vinyl ether-alt-maleic acid), Kollicoat® 100P, and Kollicoat® Protect as polymers to treat diabetic wounds and accelerate their recovery. These formulations were optimized through a series of experiments and were subsequently subjected to physicochemical tests. The results of the characterization of the dressings, microfibers, and microneedles (PMVA and 100P) were, respectively, a bioadhesion of 281.34, 720, 720, 2487, and 510.5 gf; a post-humectation bioadhesion of 186.34, 831.5, 2380, and 630.5 gf, tear strength of 2200, 1233, 1562, and 385 gf, erythema of 358, 8.4, 227, and 188; transepidermal water loss (TEWL) of 2.6, 4.7, 1.9, and 5.2 g/h·m2; hydration of 76.1, 89.9, 73.5, and 83.5%; pH of 4.85, 5.40, 5.85, and 4.85; and drug release (Peppas kinetics release) of n: 0.53, n: 0.62, n: 0.62, and n: 0.66). In vitro studies were performed on Franz-type diffusion cells and indicated flux of 57.1, 145.4, 718.7, and 2.7 µg/cm2; permeation coefficient (Kp) of 13.2, 19.56, 42, and 0.00015 cm2/h; and time lag (tL) of 6.29, 17.61, 27. 49, and 22.3 h, respectively, in wounded skin. There was no passage of ceftriaxone from dressings and microfibers to healthy skin, but that was not the case for PMVA/100P and Kollicoat® 100P microneedles, which exhibited flux of 194 and 0.4 µg/cm2, Kp of 11.3 and 0.00002 cm2/h, and tL of 5.2 and 9.7 h, respectively. The healing time of the formulations in vivo (tests carried out using diabetic Wistar rats) was under 14 days. In summary, polymeric dressings, microfibers, and microneedles loaded with ceftriaxone were developed. These formulations have the potential to address the challenges associated with chronic wounds, such as diabetic foot, improving the outcomes. Full article
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22 pages, 3430 KiB  
Article
Hydrophobic Drug Carrier from Polycaprolactone-b-Poly(Ethylene Glycol) Star-Shaped Polymers Hydrogel Blend as Potential for Wound Healing Application
by Siti Hajar Ahmad Shariff, Rusli Daik, Muhammad Salahuddin Haris and Mohamad Wafiuddin Ismail
Polymers 2023, 15(9), 2072; https://0-doi-org.brum.beds.ac.uk/10.3390/polym15092072 - 27 Apr 2023
Cited by 3 | Viewed by 1667
Abstract
Blending hydrogel with an amphiphilic polymer can increase the hydrophobic drug loading and entrapment efficiency of hydrogel-based formulations. In this study, a hydrogel formulation with star-shaped polycaprolactone-b-poly(ethylene glycol) (PCL-b-PEG) as the hydrophobic drug cargo is produced. The 4-arm and 6-arm star-shaped [...] Read more.
Blending hydrogel with an amphiphilic polymer can increase the hydrophobic drug loading and entrapment efficiency of hydrogel-based formulations. In this study, a hydrogel formulation with star-shaped polycaprolactone-b-poly(ethylene glycol) (PCL-b-PEG) as the hydrophobic drug cargo is produced. The 4-arm and 6-arm star-shaped PCL are synthesized with different molecular weights (5000, 10,000, 15,000 g/mol) via ROP and MPEG as the hydrophilic segment is attached via the Steglich esterification. FTIR and 1H-NMR analysis showed the presence of all functional groups for homopolymers and copolymers. Mn for all synthesized polymers is close to the theoretical value while GPC spectra showed a monomodal peak with narrow molecular weight distribution (PDI:1.01–1.25). The thermal degradation temperature and crystalline melting point of synthesized polymers increase with the increase in molecular weight and number of arms. All formulations possess high drug loading and entrapment efficiency (>99%) and increase with increasing molecular weight, number of arms, and amount of polymer in the formulations. All formulations showed a sustained drug release pattern with no initial burst, which follows the Korsmeyer–Peppas kinetic model. The polymer hydrogel formulations showed antibacterial activity against E. coli and S. aureus. The hydrogel containing 4-arm PCL15k-PEG is chosen as the best formulation due to its high drug release, good antimicrobial activity, and morphology. Full article
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14 pages, 4654 KiB  
Article
Electrosprayed Particles Loaded with Kartogenin as a Potential Osteochondral Repair Implant
by Sebastian J. Gurgul, Anabela Moreira, Yi Xiao, Swastina Nath Varma, Chaozong Liu, Pedro F. Costa and Gareth R. Williams
Polymers 2023, 15(5), 1275; https://0-doi-org.brum.beds.ac.uk/10.3390/polym15051275 - 2 Mar 2023
Cited by 2 | Viewed by 1867
Abstract
The restoration of cartilage damage is a slow and not always successful process. Kartogenin (KGN) has significant potential in this space—it is able to induce the chondrogenic differentiation of stem cells and protect articular chondrocytes. In this work, a series of poly(lactic-co-glycolic acid) [...] Read more.
The restoration of cartilage damage is a slow and not always successful process. Kartogenin (KGN) has significant potential in this space—it is able to induce the chondrogenic differentiation of stem cells and protect articular chondrocytes. In this work, a series of poly(lactic-co-glycolic acid) (PLGA)-based particles loaded with KGN were successfully electrosprayed. In this family of materials, PLGA was blended with a hydrophilic polymer (either polyethyleneglycol (PEG) or polyvinylpyrrolidone (PVP)) to control the release rate. Spherical particles with sizes in the range of 2.4–4.1 µm were fabricated. They were found to comprise amorphous solid dispersions, with high entrapment efficiencies of >93%. The various blends of polymers had a range of release profiles. The PLGA-KGN particles displayed the slowest release rate, and blending with PVP or PEG led to faster release profiles, with most systems giving a high burst release in the first 24 h. The range of release profiles observed offers the potential to provide a precisely tailored profile via preparing physical mixtures of the materials. The formulations are highly cytocompatible with primary human osteoblasts. Full article
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16 pages, 2230 KiB  
Article
Preparation and Optimization of Itraconazole Transferosomes-Loaded HPMC Hydrogel for Enhancing Its Antifungal Activity: 2^3 Full Factorial Design
by Eidah M. Alyahya, Knooz Alwabsi, Amal E. Aljohani, Rawan Albalawi, Mohamed El-Sherbiny, Rehab Ahmed, Yasmin Mortagi and Mona Qushawy
Polymers 2023, 15(4), 995; https://0-doi-org.brum.beds.ac.uk/10.3390/polym15040995 - 16 Feb 2023
Cited by 8 | Viewed by 2900
Abstract
Itraconazole (ITZ) is a triazole antifungal agent characterized by broad-spectrum activity against fungal infections. The main drawback of ITZ, when applied topically, is the low skin permeability due to the stratum corneum, the outermost layer of the skin, which represents the main barrier [...] Read more.
Itraconazole (ITZ) is a triazole antifungal agent characterized by broad-spectrum activity against fungal infections. The main drawback of ITZ, when applied topically, is the low skin permeability due to the stratum corneum, the outermost layer of the skin, which represents the main barrier for drug penetration. Therefore, this study aimed to prepare itraconazole as transferosomes (ITZ-TFS) to overcome the barrier function of the skin. ITZ-TFSs were prepared by thin lipid film hydration technique using different surfactants, sodium lauryl sulfate (SLS) and sodium deoxycholate (SDC). The prepared ITZ-TFS were evaluated for entrapment efficiency (EE) %, particle size, polydispersity index (PDI), zeta potential, and in vitro drug release to obtain an optimized formula. The surface morphology of the optimized formula of ITZ-TFS was determined by transmission electron microscope (TEM). The optimized formulation was prepared in the form of gel using hydroxyl propyl methyl cellulose (HPMC) gel base. The prepared ITZ-TFS gel was evaluated for homogeneity, drug content, spreadability, pH, and in vitro antifungal activity in comparison with the free ITZ gel. The prepared ITZ-TFS formulations exhibited high EE% ranging from 89.02 ± 1.65% to 98.17 ± 1.28% with particle size ranging from 132.6 ± 2.15 nm to 384.1 ± 3.46. The PDI for all ITZ-TFSs was less than 0.5 and had a negative zeta potential. The TEM image for the optimized formulation (ITZ-TFS4) showed spherical vesicles with a smooth surface. The prepared gels had good spreadability, pH, and acceptable drug content. ITZ-TFS gel showed higher antifungal activity than free ITZ gel as determined by zone of inhibition. ITZ was successfully prepared in form of TFSs with higher antifungal activity than the free drug. Full article
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12 pages, 5664 KiB  
Article
3D Printing of Triamcinolone Acetonide in Triblock Copolymers of Styrene–Isobutylene–Styrene as a Slow-Release System
by Philipp S. Hilgeroth, Justus F. Thümmler and Wolfgang H. Binder
Polymers 2022, 14(18), 3742; https://0-doi-org.brum.beds.ac.uk/10.3390/polym14183742 - 7 Sep 2022
Cited by 1 | Viewed by 1836
Abstract
Additive manufacturing has a wide range of applications and has opened up new methods of drug formulation, in turn achieving attention in medicine. We prepared styrene–isobutylene–styrene triblock copolymers (SIBS; Mn = 10 kDa–25 kDa, PDI 1,3–1,6) as a drug carrier for triamcinolone acetonide [...] Read more.
Additive manufacturing has a wide range of applications and has opened up new methods of drug formulation, in turn achieving attention in medicine. We prepared styrene–isobutylene–styrene triblock copolymers (SIBS; Mn = 10 kDa–25 kDa, PDI 1,3–1,6) as a drug carrier for triamcinolone acetonide (TA), further processed by fused deposition modeling to create a solid drug release system displaying improved bioavailability and applicability. Living carbocationic polymerization was used to exert control over block length and polymeric architecture. Thermorheological properties of the SIBS polymer (22.3 kDa, 38 wt % S) were adjusted to the printability of SIBS/TA mixtures (1–5% of TA), generating an effective release system effective for more than 60 days. Continuous drug release and morphological investigations were conducted to probe the influence of the 3D printing process on the drug release, enabling 3D printing as a formulation method for a slow-release system of Triamcinolone. Full article
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