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Pharmaceuticals
Special Issues
Applications of Surfactants in Pharmaceutical Formulation/Drug Product Development
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Applications of Surfactants in Pharmaceutical Formulation/Drug Product Development

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Pharmaceutical Technology".

Deadline for manuscript submissions: closed (31 October 2023) | Viewed by 4281

Special Issue Editors

Dr. Pradeep Kumar Bolla

E-Mail Website
Guest Editor
School of Pharmacy, The University of Texas at El Paso, 1101 N Campbell St., El Paso, TX 79902, USA
Interests: topical delivery; transdermal; permeation; IVRT; IVPT; franz cells; nanoparticles; lipid nanoparticles; skin delivery, amorphous solid dispersions, solubility enhancement
Special Issues, Collections and Topics in MDPI journals
Dr. Arun Butreddy

E-Mail Website
Guest Editor
Biologics Drug Product Development, Biogen, Cambridge, MA, USA
Interests: formulation development; solubility enhancement; lyophilization; cryoprotectants; amorphous solid dispersions; HME

Special Issue Information

Dear Colleagues,

In pharmaceutical formulation/drug product development, surfactants play a crucial role as excipients. The application of surfactants is found to be ubiquitary in biologic products. In protein formulations, surfactants are used to compete for interfaces, which can induce the unfolding and aggregation of protein molecules. In oral drug delivery, surfactants are mainly used to increase the solubility and absorption of active pharmaceutical ingredients. Several biologics such as vaccines, monoclonal antibodies, mRNA therapeutics, and gene-therapy-related products show enhanced stability in the presence of surfactants. Furthermore, formulations such as amorphous solid dispersions (ASDs) that contain surfactants have an easier processability in the case of the hot-melt extrusion process.The limitations of surfactants, such as their peroxide stability issues (biologics) and the recrystalization (ASDs) of formulations, need to be thoroughly investigated. Recent advances in this area of research have shown the potential use of surfactants in delivery to stabilize a variety of biopharmaceuticals. This Special Issue is focused on the use of surfactants in various drug delivery systems and formulations, and on their most recent advances in pharmaceutical applications.  In this Special Issue of Pharmaceuticals, the focus will be on surfactant applications for biologics, amorphous solid dispersions, suspensions, emulsions, microspheres, and other pharmaceutical applications.

Suitable topics include, but are not limited to, the following:

  • Surfactants for monoclonal antibody formulations;
  • Surfactants for vaccine formulations;
  • Surfactants for mRNA-based formulations;
  • Surfactants for amorphous solid dispersion formulations;
  • Stability issues of surfactant-based pharmaceutical formulations;
  • Surfactants for suspension formulations;
  • Surfactants for emulsion formulations;
  • Surfactants for long-acting injectable microsphere formulations.

Dr. Pradeep Kumar Bolla
Dr. Arun Butreddy
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. Pharmaceuticals 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

  • amorphous solid dispersions
  • suspensions
  • emulsions
  • microspheres
  • surfactants
  • solubility
  • solubility enhancement
  • HME

Published Papers (3 papers)

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Research

20 pages, 9886 KiB  
Article
Unveiling the Role of Nonionic Surfactants in Enhancing Cefotaxime Drug Solubility: A UV-Visible Spectroscopic Investigation in Single and Mixed Micellar Formulations
by Aysha Arshad Rana, Amnah Yusaf, Salma Shahid, Muhammad Usman, Matloob Ahmad, Sana Aslam, Sami A. Al-Hussain and Magdi E. A. Zaki
Pharmaceuticals 2023, 16(12), 1663; https://doi.org/10.3390/ph16121663 - 29 Nov 2023
Cited by 1 | Viewed by 1076
Abstract
This study reports the interfacial phenomenon of cefotaxime in combination with nonionic surfactants, Triton X-100 (TX-100) and Tween-80 (TW-80), and their mixed micellar formulations. Cefotaxime was enclosed in a micellar system to improve its solubility and effectiveness. TX-100 and TW-80 were used in [...] Read more.
This study reports the interfacial phenomenon of cefotaxime in combination with nonionic surfactants, Triton X-100 (TX-100) and Tween-80 (TW-80), and their mixed micellar formulations. Cefotaxime was enclosed in a micellar system to improve its solubility and effectiveness. TX-100 and TW-80 were used in an amphiphilic self-assembly process to create the micellar formulation. The effect of the addition of TX-100, a nonionic surfactant, on the ability of TW-80 to solubilize the drug was examined. The values of the critical micelle concentration (CMC) were determined via UV-Visible spectroscopy. Gibbs free energies (ΔGp and ΔGb), the partition coefficient (Kx), and the binding constant (Kb) were also computed. In a single micellar system, the partition coefficient (Kx) was found to be 33.78 × 106 and 2.78 × 106 in the presence of TX-100 and TW-80, respectively. In a mixed micellar system, the value of the partition coefficient for the CEF/TW-80 system is maximum (5.48 × 106) in the presence of 0.0019 mM of TX-100, which shows that TX-100 significantly enhances the solubilizing power of micelles. It has been demonstrated that these surfactants are effective in enhancing the solubility and bioavailability of therapeutic compounds. This study elaborates on the physicochemical characteristics and solubilization of reactive drugs in single and mixed micellar media. This investigation, conducted in the presence of surfactants, shows a large contribution to the binding process via both hydrogen bonding and hydrophobic interactions. Full article
(This article belongs to the Special Issue Applications of Surfactants in Pharmaceutical Formulation/Drug Product Development)
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16 pages, 5118 KiB  
Article
Development and Evaluation of Solid Dispersion-Based Sublingual Films of Nisoldipine
by Yahya Alhamhoom, Abhay Sharma, Shivakumar Hagalavadi Nanjappa, Avichal Kumar, Anas Alshishani, Mohammed Muqtader Ahmed, Syeda Ayesha Farhana and Mohamed Rahamathulla
Pharmaceuticals 2023, 16(11), 1589; https://doi.org/10.3390/ph16111589 - 09 Nov 2023
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Abstract
Nisoldipine (NIS) is a calcium channel blocker that exhibits poor bioavailability (~5%) due to low aqueous solubility and presystemic metabolism in the gut wall. In this context, the present work aimed to develop NIS solid dispersion (NISSD)-based sublingual films using solvent casting technique [...] Read more.
Nisoldipine (NIS) is a calcium channel blocker that exhibits poor bioavailability (~5%) due to low aqueous solubility and presystemic metabolism in the gut wall. In this context, the present work aimed to develop NIS solid dispersion (NISSD)-based sublingual films using solvent casting technique to improve the dissolution. Phase solubility studies indicated that Soluplus® was the most effective carrier for improving the aqueous solubility of NIS. NISSDs were initially developed using the solvent evaporation method. Fourier transform infrared spectrometric studies were found to display the characteristic vibrational bands related to C=O stretching and N-H deformation in NISSDs, proving the chemical integrity of the drug in NISSDs. Subsequently, bioadhesive sublingual films of NISSDs were formulated using solvent casting method, using hydroxypropyl methyl cellulose (HPMC) E5, E15, and hydroxy ethyl cellulose (HEC EF) as hydrophilic polymers and polyethylene glycol 400 (PEG 400) as plasticizer. The incorporation of NISSDs was found to produce clear films that displayed uniform content. The sublingual film of NISSDs composed of HPMC E5 (2% w/v), was found to display the least thickness (0.29 ± 0.02 mm), the highest folding endurance (168.66 ± 4.50 times), and good bioadhesion strength (12.73 ± 0.503 g/cm2). This film was found to rapidly disintegrate (28.66 ± 3.05 sec) and display near-complete drug release (94.24 ± 1.22) in 30 min. Incorporating NISSDs into rapidly bioadhesive sublingual films considerably improves drug dissolution. Overall, these research outcomes underscored the potential of rapidly dissolving bioadhesive sublingual films to evade gut metabolism and resolve the bioavailability issues associated with oral administration of NIS. Full article
(This article belongs to the Special Issue Applications of Surfactants in Pharmaceutical Formulation/Drug Product Development)
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18 pages, 1792 KiB  
Article
Influence of Extrudate-Based Textural Properties on Pellet Molding Quality
by Wenxiu Tian, Xue Li, Wenjie Li, Aile Xue, Minyue Zheng, Xiao Lin and Yanlong Hong
Pharmaceuticals 2023, 16(10), 1505; https://doi.org/10.3390/ph16101505 - 23 Oct 2023
Viewed by 1114
Abstract
As the precursor of pellets, the extrudate has a direct impact on the molding quality of the pellets. Therefore, the correlation between the surface roughness of the extrudates and the molding quality of pellets with pure microcrystalline cellulose (MCC) formulations and those containing [...] Read more.
As the precursor of pellets, the extrudate has a direct impact on the molding quality of the pellets. Therefore, the correlation between the surface roughness of the extrudates and the molding quality of pellets with pure microcrystalline cellulose (MCC) formulations and those containing traditional Chinese medicine (TCM) formulations was explored. MCC was used as a pelleting agent, mixer torque rheometry (MTR) was used to guide the optimal dosage of the wetting agent, and TCM extracts (drug loadings of 20% to 40%) were selected as model drugs to prepare the extrudates and pellets under the same extrusion spheronization process conditions. The surface roughness and texture parameters of extrudates were analyzed via a microscope and texture analyzer, respectively, and the quality of pellets was evaluated. The extrudate roughness of the pure MCC prescription decreased and then increased with increasing water addition, while the extrudate roughness of the prescription containing TCM extracts tended to increase and then decrease. The addition of water affected the extrudate properties, with TCM extract molecules filling gaps in the MCC structure, leading to rough surfaces. The extrudate roughness of the TCM prescriptions was significantly greater than that of the pure MCC prescriptions at optimal water addition levels, resulting in ideal pellets. Full article
(This article belongs to the Special Issue Applications of Surfactants in Pharmaceutical Formulation/Drug Product Development)
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