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Pharmaceutics
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Research on Hot Melt Extrusion Processing for Drug Formulation and...
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Research on Hot Melt Extrusion Processing for Drug Formulation and Drug Delivery

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Pharmaceutical Technology, Manufacturing and Devices".

Deadline for manuscript submissions: closed (20 July 2024) | Viewed by 5915

Special Issue Editors

Dr. Sateesh Kumar Vemula

E-Mail Website
Guest Editor
Department of Pharmaceutics and Drug Delivery, School of Pharmacy, The University of Mississippi, Oxford, MS 38677, USA
Interests: hot-melt extrusion; colon-specific drug delivery; fast-dissolving tablets; formulation and pharmacokinetics
Prof. Dr. Michael A. Repka

E-Mail Website
Guest Editor
Distinguished Professor, Department of Pharmaceutics and Drug Delivery, University of Mississippi, University, MS 38677, USA
Interests: hot-melt extrusion (HME) for enhancing solubility and bioavailability of poorly soluble drugs; pharmaceutical novel dosage forms and devices; HME and fused deposition modeling for complex patient centric delivery to pediatric, geriatric and special needs patients; polymeric drug delivery design and stabilization; formulation and process development for natural products; antifungal/antibacterial agents; research on several drug delivery areas including oral, transdermal/trans-nail, nose-to-brain, and transcorneal delivery
Special Issues, Collections and Topics in MDPI journals
Dr. Naveen Chella

E-Mail Website
Guest Editor
Department of Pharmaceutical Technology (Formulations), National Institute of Pharmaceutical Education and Research (NIPER), Guwahati, Assam 781101, India
Interests: hot-melt extrusion; melt granulation; lipid-based DDS; topical formulations; solid dispersions

Special Issue Information

Dear Colleagues,

The pharmaceutical industry has shown increased interest in hot-melt extrusion (HME) technology, as evidenced by a rise in patents and publications. HME is becoming popular in pharmaceutical applications to develop various drug delivery systems due to its eco-friendly approach to continuous manufacturing without solvents. HME has proven very efficient in enhancing the solubility and dissolution of poorly water-soluble drugs via the development of amorphous solid dispersions. During the process, the active pharmaceutical ingredient is mixed at a molecular level with thermoplastic binders and/or polymers while passing through high-temperature counter-rotating or corotating screw elements. This molecular mixing process transforms the active pharmaceutical ingredient into an amorphous form and improves the dissolution rate. Additionally, it is an essential tool for producing innovative pharmaceutical products. HME is being investigated as an alternative technology for preparing multicomponent systems such as co-crystals and co-amorphous techniques. Twin-screw granulation has drawn increased attention in preparing granules via twin-screw melt or dry granulation.

We welcome submissions from researchers exploring hot-melt extrusion processing for drug formulation and delivery.

The purpose of this Special Issue, "Research on Hot Melt Extrusion Processing for Drug Formulation and Drug Delivery" is to gather original research articles and reviews on the formulation and in-vitro/in-vivo characterization of various drug delivery systems such as amorphous solid dispersions, co-crystals, SEEDS, and any other fast-dissolving systems using hot-melt extrusion. It also works using modified-release systems such as controlled-release tablets/implants/pellets, colon-specific delivery, gastroretentive systems, and mucoadhesive systems via the application of hot-melt extrusion. Works aimed at increasing the application of HME knowledge to improve dissolution rates or bioavailability in order to enhance overall therapeutic efficacy are welcome.

We look forward to receiving your contributions.

Dr. Sateesh Kumar Vemula
Prof. Dr. Michael A. Repka
Dr. Naveen Chella
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

  • hot-melt extrusion (HME)
  • pharmaceutical industry
  • twin-screw granulation
  • continuous manufacturing
  • drug delivery
  • solubility and dissolution
  • amorphous form
  • bioavailability
  • formulation and development
  • in-vitro/in-vivo characterization

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Published Papers (4 papers)

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Research

12 pages, 7365 KiB  
Article
Dry Amorphization of Itraconazole Using Mesoporous Silica and Twin-Screw Technology
by Margarethe Richter, Simon Welzmiller, Fred Monsuur, Annika R. Völp and Joachim Quadflieg
Pharmaceutics 2024, 16(11), 1368; https://doi.org/10.3390/pharmaceutics16111368 - 25 Oct 2024
Viewed by 595
Abstract
Background/Objectives: Amorphization of an active pharmaceutical ingredient (API) can improve its dissolution and enhance bioavailability. Avoiding solvents for drug amorphization is beneficial due to environmental issues and potential solvent residues in the final product. Methods: Dry amorphization using a twin-screw extruder is presented [...] Read more.
Background/Objectives: Amorphization of an active pharmaceutical ingredient (API) can improve its dissolution and enhance bioavailability. Avoiding solvents for drug amorphization is beneficial due to environmental issues and potential solvent residues in the final product. Methods: Dry amorphization using a twin-screw extruder is presented in this paper. A blend of mesoporous silica particles and crystalline itraconazole was processed using a pharma-grade laboratory scale twin-screw extruder. The influence of different screw configurations and process parameters was tested. Particle size and shape are compared in scanning electron microscopy (SEM) images. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) are used to determine the residual amount of crystalline itraconazole in the final product. Results: An optimized screw configuration for the process was found which leads to more than 90% amorphous API when processed at room temperature. Full amorphization was reached at 70 °C. The specific mechanic energy (SME) introduced into the material during twin-screw processing is crucial for the dry amorphization. The higher the SME, the lower the residual amount of crystalline API. Two months after processing, however, recrystallization was observed by XRD. Conclusions: Dry processing using a twin-screw extruder is continuous, free of solvents and can be performed at low temperatures. This study proves the concept of twin-screw processing with mesoporous silica for dry amorphization of itraconazole. Full article
(This article belongs to the Special Issue Research on Hot Melt Extrusion Processing for Drug Formulation and Drug Delivery)
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20 pages, 3989 KiB  
Article
Quality by Design (QbD) Approach to Develop Colon-Specific Ketoprofen Hot-Melt Extruded Pellets: Impact of Eudragit® S 100 Coating on the In Vitro Drug Release
by Sateesh Kumar Vemula, Sagar Narala, Prateek Uttreja, Nagarjuna Narala, Bhaskar Daravath, Chamundeswara Srinivasa Akash Kalla, Srikanth Baisa, Siva Ram Munnangi, Naveen Chella and Michael A. Repka
Pharmaceutics 2024, 16(10), 1265; https://doi.org/10.3390/pharmaceutics16101265 - 27 Sep 2024
Viewed by 706
Abstract
Background: A pelletizer paired with hot-melt extrusion technology (HME) was used to develop colon-targeted pellets for ketoprofen (KTP). Thermal stability and side effects in the upper gastrointestinal tract made ketoprofen more suitable for this work. Methods: The pellets were prepared using the enzyme-triggered [...] Read more.
Background: A pelletizer paired with hot-melt extrusion technology (HME) was used to develop colon-targeted pellets for ketoprofen (KTP). Thermal stability and side effects in the upper gastrointestinal tract made ketoprofen more suitable for this work. Methods: The pellets were prepared using the enzyme-triggered polymer Pectin LM in the presence of HPMC HME 4M, followed by pH-dependent Eudragit® S 100 coating to accommodate the maximum drug release in the colon by minimizing drug release in the upper gastrointestinal tract (GIT). Box–Behnken Design (BBD) was used for response surface optimization of the proportion of different independent variables like Pectin LM (A), HPMC HME 4M (B), and Eudragit® S 100 (C) required to lower the early drug release in upper GIT and to extend the drug release in the colon. Results: Solid-state characterization studies revealed that ketoprofen was present in a solid solution state in the hot-melt extruded polymer matrix. The desired responses of the prepared optimized KTP pellets obtained by considering the designed space showed 1.20% drug release in 2 h, 3.73% in the first 5 h of the lag period with the help of Eudragit® S 100 coating, and 93.96% in extended release up to 24 h in the colonic region. Conclusions: Hence, developing Eudragit-coated hot-melt extruded pellets could be a significant method for achieving the colon-specific release of ketoprofen. Full article
(This article belongs to the Special Issue Research on Hot Melt Extrusion Processing for Drug Formulation and Drug Delivery)
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28 pages, 10826 KiB  
Article
QbD-Based Development and Evaluation of Pazopanib Hydrochloride Extrudates Prepared by Hot-Melt Extrusion Technique: In Vitro and In Vivo Evaluation
by Amit Gupta, Rashmi Dahima, Sunil K. Panda, Annie Gupta, Gaurav Deep Singh, Tanveer A. Wani, Afzal Hussain and Devashish Rathore
Pharmaceutics 2024, 16(6), 764; https://doi.org/10.3390/pharmaceutics16060764 - 4 Jun 2024
Cited by 1 | Viewed by 1324
Abstract
Background: Pazopanib hydrochloride (PZB) is a protein kinase inhibitor approved by the United States Food and Drug Administration and European agencies for the treatment of renal cell carcinoma and other renal malignancies. However, it exhibits poor aqueous solubility and inconsistent oral drug absorption. [...] Read more.
Background: Pazopanib hydrochloride (PZB) is a protein kinase inhibitor approved by the United States Food and Drug Administration and European agencies for the treatment of renal cell carcinoma and other renal malignancies. However, it exhibits poor aqueous solubility and inconsistent oral drug absorption. In this regard, the current research work entails the development and evaluation of the extrudates of pazopanib hydrochloride by the hot-melt extrusion (HME) technique for solubility enhancement and augmenting oral bioavailability. Results: Solid dispersion of the drug was prepared using polymers such as Kollidon VA64, hydroxypropylmethylcellulose (HPMC), Eudragit EPO, and Affinisol 15LV in a 1:2 ratio by the HME process through a lab-scale 18 mm extruder. Systematic optimization of the formulation variables was carried out with the help of custom screening design (JMP Software by SAS, Version 14.0) to study the impact of polymer type and plasticizer level on the quality of extrudate processability by measuring the torque value, appearance, and disintegration time as the responses. The polymer blends containing Kollidon VA64 and Affinisol 15LV resulted in respective clear transparent extrudates, while Eudragit EPO and HPMC extrudates were found to be opaque white and brownish, respectively. Furthermore, evaluation of the impact of process parameters such as screw rpm and barrel temperature was measured using a definitive screening design on the extrude appearance, torque, disintegration time, and dissolution profile. Based on the statistical outcomes, it can be concluded that barrel temperature has a significant impact on torque, disintegration time, and dissolution at 30 min, while screw speed has an insignificant impact on the response variables. Affinisol extrudates showed less moisture uptake and faster dissolution in comparison to Kollidon VA64 extrudates. Affinisol extrudates were evaluated for polymorphic stability up to a 3-month accelerated condition and found no recrystallization. PZB–Extrudates using the Affinisol polymer (Test formulation A) revealed significantly higher bioavailability (AUC) in comparison to the free Pazopanib drug and marketed formulation. Full article
(This article belongs to the Special Issue Research on Hot Melt Extrusion Processing for Drug Formulation and Drug Delivery)
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25 pages, 4065 KiB  
Article
Material-Sparing Feasibility Screening for Hot Melt Extrusion
by Amanda Pluntze, Scott Beecher, Maria Anderson, Dillon Wright and Deanna Mudie
Pharmaceutics 2024, 16(1), 76; https://doi.org/10.3390/pharmaceutics16010076 - 5 Jan 2024
Viewed by 2044
Abstract
Hot melt extrusion (HME) offers a high-throughput process to manufacture amorphous solid dispersions. A variety of experimental and model-based approaches exist to predict API solubility in polymer melts, but these methods are typically aimed at determining the thermodynamic solubility and do not take [...] Read more.
Hot melt extrusion (HME) offers a high-throughput process to manufacture amorphous solid dispersions. A variety of experimental and model-based approaches exist to predict API solubility in polymer melts, but these methods are typically aimed at determining the thermodynamic solubility and do not take into account kinetics of dissolution or the associated degradation of the API during thermal processing, both of which are critical considerations in generating a successful amorphous solid dispersion by HME. This work aims to develop a material-sparing approach for screening manufacturability of a given pharmaceutical API by HME using physically relevant time, temperature, and shear. Piroxicam, ritonavir, and phenytoin were used as model APIs with PVP VA64 as the dispersion polymer. We present a screening flowchart, aided by a simple custom device, that allows rapid formulation screening to predict both achievable API loadings and expected degradation from an HME process. This method has good correlation to processing with a micro compounder, a common HME screening industry standard, but only requires 200 mg of API or less. Full article
(This article belongs to the Special Issue Research on Hot Melt Extrusion Processing for Drug Formulation and Drug Delivery)
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