Pharmaceutics最新文献

{"title":"The Role of Natural Deep Eutectic Solvents in a Hydrogel Formulation Containing Lidocaine.","authors":"Feria Hasanpour, Mária Budai-Szűcs, Anita Kovács, Rita Ambrus, Orsolya Jójárt-Laczkovich, Boglárka Szalai, Branimir Pavlić, Péter Simon, Levente Törteli, Szilvia Berkó","doi":"10.3390/pharmaceutics17030324","DOIUrl":"10.3390/pharmaceutics17030324","url":null,"abstract":"<p><p><b>Background/Objectives</b>: This study investigates the use of natural deep eutectic solvents (NADESs) in enhancing the solubility and skin permeation of a lidocaine base, a lipophilic form, in hydrogel systems. The aim was to develop an environmentally sustainable and biocompatible alternative to conventional lidocaine formulations, improving the dermal permeation and therapeutic efficacy. <b>Methods:</b> The lidocaine base was dissolved in a hydrophilic NADES system composed of choline chloride and citric acid, facilitating enhanced solubility, likely through new molecular interactions. Then, pH-adjusted hydrogels were formulated and optimized by employing a 3² full factorial design. Raman and nuclear magnetic resonance (NMR) spectroscopy were applied to evaluate the stability of lidocaine in the optimal formulation. The biopharmaceutical properties were investigated using in vitro drug release and skin permeation studies. In vivo tests assessed physiological skin parameters such as the hydration and transepidermal water loss. <b>Results:</b> The developed NADES-containing hydrogel significantly improved the solubility and stability of lidocaine. Skin permeation studies demonstrated enhanced dermal permeation compared with conventional hydrogel and ointment. These improvements, namely the enhanced solubility of lidocaine in the formulation and its increased permeation, were attributed to the dual effect of the NADES. <b>Conclusions:</b> NADES-containing hydrogels represent a promising green technology for formulating lidocaine-containing dermal preparations. This approach offers a biocompatible, natural-based alternative that can enhance the bioavailability and efficacy of topical anesthetics.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 3","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-03-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11944536/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143720996","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Pharmacogenetic Influences on Individual Responses to Ocular Hypotensive Agents in Glaucoma Patients.","authors":"Sara Labay-Tejado, Virginia Fortuna, Néstor Ventura-Abreu, Mar Hernaez, Valeria Opazo-Toro, Alba Garcia-Humanes, Mercè Brunet, Elena Milla","doi":"10.3390/pharmaceutics17030325","DOIUrl":"10.3390/pharmaceutics17030325","url":null,"abstract":"<p><p><b>Background/Objectives</b>: To analyze the genotype that predicts the phenotypic characteristics of a cohort of patients with glaucoma and ocular hypertension (OHT) and explore their influence on the response to ocular hypotensive treatment. <b>Methods</b>: This was a prospective study that included 193 eyes of 109 patients with glaucoma or OHT under monotherapy with beta-blockers, prostaglandin, or prostamide analogues (BBs, PGAs, PDs). Eight single-nucleotide polymorphisms were genotyped using real-time PCR assays: prostaglandin-F2α receptor (<i>PTGFR</i>) (rs3766355, rs3753380); beta-2-adrenergic receptor (<i>ADRB2</i>) (rs1042714); and cytochrome P450 2D6 (<i>CYP2D6</i>) (<i>*2</i> rs16947; <i>*35</i> rs769258; <i>*4</i> rs3892097; <i>*9</i> rs5030656, and <i>*41</i> rs28371725). The main variables studied were baseline (bIOP), treated (tIOP), and rate of variation in intraocular pressure (vIOP), and mean deviation of the visual field (MD). The metabolizer phenotype and the <i>CYP2D6</i> copy number variation were also evaluated. <b>Results</b>: In total, 112 eyes were treated with PGAs (58.0%), 59 with BBs (30.6%), and 22 with PDs (11.4%). For <i>PTGFR</i> (rs3753380), statistically significant differences were observed in vIOP in the PGA group (<i>p</i> = 0.032). Differences were also observed for <i>ADRB2</i> (rs1042714) in MD (<i>p</i> < 0.001) and vIOP (<i>p</i> = 0.017). For <i>CYP2D6</i>, ultrarapid metabolizers exhibited higher tIOP (<i>p</i> = 0.010) and lower vIOP (<i>p</i> = 0.046) compared to the intermediate and poor metabolizers of the BB group. Additionally, systemic treatment metabolized by <i>CYP2D6</i> showed a significant influence on vIOP (<i>p</i> = 0.019) in this group. <b>Conclusions</b>: These preliminary findings suggest the future potential of pharmacogenetic-based treatments in glaucoma to achieve personalized treatment for each patient, and thus optimal clinical management.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 3","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-03-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11944811/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143721049","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"An Investigation into the Effect of Maltitol, Sorbitol, and Xylitol on the Formation of Carbamazepine Solid Dispersions Through Thermal Processing.","authors":"Madan Sai Poka, Marnus Milne, Anita Wessels, Marique Aucamp","doi":"10.3390/pharmaceutics17030321","DOIUrl":"10.3390/pharmaceutics17030321","url":null,"abstract":"<p><p><b>Background:</b> Carbamazepine (CBZ) is a Biopharmaceutical Classification System (BCS) class II drug, that is practically insoluble in water, influencing the oral bioavailability. Polyols are highly hydrophilic crystalline carriers studied for their success in developing solid dispersions (SDs) for improved solubility and dissolution rate. Polyols are generally regarded as safe (GRAS) and maltitol (MAL), xylitol (XYL) and sorbitol (SOR) are among the approved polyols for market use. While xylitol (XYL) and sorbitol, have shown promise in improving the solubility and dissolution rates of poorly soluble drugs, their full potential in the context of improving the solubility of carbamazepine have not been thoroughly investigated. To the best of our knowledge, maltitol (MAL) was not studied previously as a carrier for preparing SDs. Hence, the purpose of this study was to investigate their use in the preparation of CBZ SDs by the fusion method. <b>Methods:</b> CBZ-polyol SDs were prepared in varying molar ratios (2:1, 1:1 and 1:2) and characterised for solid-state nature, solubility and in-vitro dissolution rate. <b>Results:</b> Solid-state characterisation of the CBZ-polyol SDs revealed the existence of the SDs as continuous glass suspensions with fine CBZ crystallites suspended in the amorphous polyol carriers. Among the polyols studied, XYL exhibited good miscibility with CBZ and showed significant improvement in the solubility and dissolution rate. The prepared SDs showed a 2 to 6-folds increase in CBZ solubility and 1.4 to 1.9-folds increase in dissolution rate in comparison with pure CBZ. <b>Conclusions:</b> The study explains the possible use of polyols (XYL and SOR) based SDs of BCS Class II drugs with good glass forming ability for enhanced solubility and dissolution.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 3","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-03-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11946217/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143720981","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Sanguinarine-Chelerythrine from <i>Coptis chinensis</i> Offers Analgesic and Anti-Inflammatory Effects Without Gastrotoxicity.","authors":"Maciej Danielewski, Sylwia Zielińska, Anna Merwid-Ląd, Marta Szandruk-Bender, Wojciech Słupski, Maciej Włodarczyk, Tomasz Sozański, Piotr Ziółkowski, Adam Szeląg, Beata Nowak","doi":"10.3390/pharmaceutics17030323","DOIUrl":"10.3390/pharmaceutics17030323","url":null,"abstract":"<p><p><b>Background</b>: Pain is a major clinical and socioeconomic problem worldwide. The available therapies are not always effective and are often associated with the multiple adverse effects that reduce their clinical application. Natural compounds are an important group of pharmaceuticals that may be used in pain management. We aimed to investigate the analgesic activity of the sanguinarine-chelerythrine from <i>Coptis chinensis</i>. <b>Methods</b>: The analgesic and anti-inflammatory activity of the sanguinarine-chelerythrine fraction of <i>C. chinensis</i> extract (SC 5 and 10 mg/kg), sanguinarine (SAN 1 and 2 mg/kg) and chelerythrine (CHEL 4 and 8 mg/kg) was assessed in tail flick and formalin tests. A microscopic and macroscopic examination of stomach mucosae was performed. TNFα and MMP-9 levels were measured with ELISA kits. <b>Results</b>: Morphine (MORF), CHEL and SC prolongated the tail withdrawal latency, with comparable analgesic activity between MORF and CHEL 8 mg/kg. MORF, CHEL 8 mg/kg, and SAN 2 mg/kg ameliorated the pain reaction in the neurogenic phase of the formalin test. In the inflammatory phase of the formalin test, all tested substances exerted analgesic activity. SAN, CHEL and SC additionally reduced TNFα and MMP-9 secretion. <b>Conclusions</b>: Our results confirmed analgesic effects of CHEL and SC with CHEL analgesic activity comparable to MORF. All investigated substances exerted significant anti-inflammatory activity without concomitant gastrotoxicity.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 3","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-03-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11946437/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143721001","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A Formulation-Process-Product Integrated Design Method for Accelerating Pharmaceutical Tablet Development via the High-Shear Wet Granulation and Tableting Route.","authors":"Zichen Liang, Xuefang Tang, Liping Chen, Yifei Liu, Shuying Zhao, Xiao Ma, Gan Luo, Bing Xu","doi":"10.3390/pharmaceutics17030322","DOIUrl":"10.3390/pharmaceutics17030322","url":null,"abstract":"<p><p><b>Background/Objectives</b>: Tablet is the most popular oral solid dosage form, and high-shear wet granulation and tableting (HSWGT) is a versatile technique for manufacturing tablets. The conventional pharmaceutical development for HSWGT is carried out in a step-by-step mode, which is inefficient and may result in local optimal solutions. Inspired by the co-design philosophy, a formulation-process-product integrated design (FPPID) framework is innovatively brought forward to enable the target-oriented and simultaneous exploration of the formulation design space and the process design space. <b>Methods</b>: A combination of strategies, such as a material library, model-driven design (MDD), and simulation-supported solution generation, are used to manage the complexity of the multi-step development processes of HSWGT. The process model was developed at the intermediate level by incorporating dimensionless parameters from the wet granulation regime map approach into the process of the partial least square (PLS) model. The tablets tensile strength (<i>TS</i>) and solid fraction (<i>SF</i>) could be predicted from the starting materials' properties and process parameters. The material library was used to diversify the model input and improve the model's generalization ability. Furtherly, the mixture properties calculation model and the process model were interconnected. <b>Results</b>: A four-step FPPID methodology including the target definition, the formulation simulation, the process simulation, and the solution generation was implemented. The performance of FPPID was demonstrated through the efficient development of high-drug-loading tablets. <b>Conclusions</b>: As a holistic design method, the proposed FPPID offers great opportunity for designers to handle the complex interplay in the sequential development stages, facilitate instant decisions, and accelerate product development.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 3","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-03-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11944958/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143720891","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Assessing Drug-Drug Interaction and Food Effect for BCS Class 2 Compound BI 730357 (Retinoic Acid-Related Orphan Receptor Gamma Antagonist, Bevurogant) Using a Physiology-Based Pharmacokinetics Modeling (PBPK) Approach with Semi-Mechanistic Absorption.","authors":"Tobias Kanacher, Erik Sjögren, Julia Korell, Elodie L Plan, Jose David Gómez-Mantilla, Ibrahim Ince","doi":"10.3390/pharmaceutics17030314","DOIUrl":"10.3390/pharmaceutics17030314","url":null,"abstract":"<p><p><b>Background</b>: The drug candidate BI 730357 is a Biopharmaceutics Classification System (BCS) Class II compound showing atypical absorption after oral administration in fasted and fed healthy individuals, for which conventional traditional deconvolution methods could not explain formulation dependencies. <b>Methods</b>: A physiologically based pharmacokinetic (PBPK) model of BI 730357 was developed using the Open Systems Pharmacology (OSP) PBPK software tool PK-Sim^®, which could describe the pharmacokinetics in fasted and fed subjects after single and multiple doses. A Weibull function was used to describe the in vivo formulation kinetics, whereas colonic absorption was adopted as the main driver to describe the late phases of observed pharmacokinetics after oral administration. The food effect was applied using the implemented feature PK-Sim^®. <b>Results</b>: The model accurately predicted an observed itraconazole drug-drug interaction (DDI) in fasted subjects and was used to explore the effects of the strong CYP3A4 inducer rifampicin on the pharmacokinetics of BI 730357 after administration in fed subjects. <b>Conclusions</b>: The combined results suggest that the BI 730357 PBPK model with semi-mechanistic absorption can prospectively explore the effects of CYP3A4 inhibitors and inducers on the pharmacokinetics after administration in fed or fasted subjects within the given dose range.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 3","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11945243/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143720992","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Computer-Aided Drug Design in Research on Chinese Materia Medica: Methods, Applications, Advantages, and Challenges.","authors":"Ban Chen, Shuangshuang Liu, Huiyin Xia, Xican Li, Yingqing Zhang","doi":"10.3390/pharmaceutics17030315","DOIUrl":"10.3390/pharmaceutics17030315","url":null,"abstract":"<p><p>Chinese materia medica (CMM) refers to the medicinal substances used in traditional Chinese medicine. In recent years, CMM has become globally prevalent, and scientific research on CMM has increasingly garnered attention. Computer-aided drug design (CADD) has been employed in Western medicine research for many years, contributing significantly to its progress. However, the role of CADD in CMM research has not been systematically reviewed. This review briefly introduces CADD methods in CMM research from the perspectives of computational chemistry (including quantum chemistry, molecular mechanics, and quantum mechanics/molecular mechanics) and informatics (including cheminformatics, bioinformatics, and data mining). Then, it provides an exhaustive discussion of the applications of these CADD methods in CMM research through rich cases. Finally, the review outlines the advantages and challenges of CADD in CMM research. In conclusion, despite the current challenges, CADD still offers unique advantages over traditional experiments. With the development of the CMM industry and computer science, especially driven by artificial intelligence, CADD is poised to play an increasingly pivotal role in advancing CMM research.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 3","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11945071/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143721012","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Towards DFO*¹²-Preliminary Results of a New Chelator for the Complexation of Actinium-225.","authors":"Irene V J Feiner, Dennis Svatunek, Martin Pressler, Tori Demuth, Xabier Guarrochena, Johannes H Sterba, Susanne Dorudi, Clemens Pichler, Christoph Denk, Thomas L Mindt","doi":"10.3390/pharmaceutics17030320","DOIUrl":"10.3390/pharmaceutics17030320","url":null,"abstract":"<p><p><b>Background</b>: Actinium-225 (²²⁵Ac) has gained interest in nuclear medicine for use in targeted alpha therapy (TAT) for the treatment of cancer. However, the number of suitable chelators for the stable complexation of ²²⁵Ac³⁺ is limited. The promising physical properties of ²²⁵Ac result in an increased demand for the radioisotope that is not matched by its current supply. To expand the possibilities for the development of ²²⁵Ac-based TAT therapeutics, a new hydroxamate-based chelator, DFO*¹², is described. We report the DFT-guided design of dodecadentate DFO*¹² and an efficient and convenient automated solid-phase synthesis for its preparation. To address the limited availability of ²²⁵Ac, a small-scale ²²⁹Th/²²⁵Ac generator was constructed in-house to provide [²²⁵Ac]AcCl₃ for research. <b>Methods</b>: DFT calculations were performed in ORCA 5.0.1 using the BP86 functional with empirical dispersion correction D3 and Becke-Johnson damping (D3BJ). The monomer synthesis over three steps enabled the solid-phase synthesis of DFO*¹². The small-scale ²²⁹Th/²²⁵Ac generator was realized by extracting ²²⁹Th from aged ²³³U material. Radiolabeling of DFO*¹² with ²²⁵Ac was performed in 1 M TRIS pH 8.5 or 1.5 M NaOAc pH 4.5 for 30 min at 37 °C. <b>Results</b>: DFT calculations directed the design of a dodecadentate chelator. The automated synthesis of the chelator DFO*¹² and the development of a small-scale ²²⁹Th/²²⁵Ac generator allowed for the radiolabeling of DFO*¹² with ²²⁵Ac quantitatively at 37 °C within 30 min. The complex [²²⁵Ac]Ac-DFO*¹² indicated good stability in different media for 20 h. <b>Conclusions</b>: The novel hydroxamate-based dodecadentate chelator DFO*¹², together with the developed ²²⁹Th/²²⁵Ac generator, provide new opportunities for ²²⁵Ac research for future radiopharmaceutical development and applications in TAT.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 3","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11946154/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143721016","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Novel HSA-PMEMA Nanomicelles Prepared via Site-Specific In Situ Polymerization-Induced Self-Assembly for Improved Intracellular Delivery of Paclitaxel.","authors":"Yang Chen, Shuang Liang, Binglin Chen, Fei Jiao, Xuliang Deng, Xinyu Liu","doi":"10.3390/pharmaceutics17030316","DOIUrl":"10.3390/pharmaceutics17030316","url":null,"abstract":"<p><p><b>Background/Objectives</b>: Paclitaxel (PTX) is a potent anticancer drug that is poorly soluble in water. To enhance its delivery efficiency in aqueous environments, amphiphilic polymer micelles are often used as nanocarriers for PTX in clinical settings. However, the hydrophilic polymer segments on the surface of these micelles may possess potential immunogenicity, posing risks in clinical applications. To address this issue, nanomicelles based on human serum albumin (HSA)-hydrophobic polymer conjugates constructed via site-specific in situ polymerization-induced self-assembly (SI-PISA) are considered a promising alternative. The HSA shell not only ensures good biocompatibility but also enhances cellular uptake because of endogenous albumin trafficking pathways. Moreover, compared to traditional methods of creating protein-hydrophobic polymer conjugates, SI-PISA demonstrates higher reaction efficiency and better preservation of protein functionality. <b>Methods</b>: We synthesized HSA-PMEMA nanomicelles via SI-PISA using HSA and methoxyethyl methacrylate (MEMA)-a novel hydrophobic monomer with a well-defined and stable chemical structure. The protein activity and the PTX intracellular delivery efficiency of HSA-PMEMA nanomicelles were evaluated. <b>Results</b>: The CD spectra of HSA and HSA-PMEMA exhibited similar shapes, and the relative esterase-like activity of HSA-PMEMA was 94% that of unmodified HSA. Flow cytometry results showed that Cy7 fluorescence intensity in cells treated with HSA-PMEMA-Cy7 was approximately 1.35 times that in cells treated with HSA-Cy7; meanwhile, HPLC results indicated that, under the same conditions, the PTX loading per unit protein mass on HSA-PMEMA was approximately 1.43 times that of HSA. These collectively contributed to a 1.78-fold overall PTX intracellular delivery efficiency of HSA-PMEMA compared to that of HSA. <b>Conclusions</b>: In comparison with HSA, HSA-PMEMA nanomicelles exhibit improved cellular uptake and higher loading efficiency for PTX, effectively promoting the intracellular delivery of PTX. Tremendous potential lies in these micelles for developing safer and more efficient next-generation PTX formulations for tumor treatment.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 3","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11945012/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143721037","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Assessment of the Anti-Acne Properties of Some Medicinal Plants and Development of an Herbal Anti-Acne Formulation.","authors":"F Sezer Senol Deniz, Ozlem Oyardı, Cagla Bozkurt Guzel, Tahir Emre Yalcın, Serkan Yiğitkan, Yuksel Kan, Nurver Ulger Toprak, Ilkay Erdogan Orhan","doi":"10.3390/pharmaceutics17030317","DOIUrl":"10.3390/pharmaceutics17030317","url":null,"abstract":"<p><p><b>Background</b>: Acne is a prevalent dermatological condition characterized by the blockage of hair follicles and sebaceous glands, leading to the formation of acne. The anaerobe pathogen <i>Cutibacterium acnes</i> (formerly known as <i>Propionibacterium acnes</i>) plays an essential role in the pathogenesis of acne, for which generally antimicrobial treatment is required. Acne is a substantial health concern, and continuing research is being conducted to discover novel and efficacious remedies. The antimicrobial activity of plants has been demonstrated in numerous studies, and they are still targeted organisms in drug development. Studies showing that plants are effective against acne pathogens have also been reported. <b>Methods</b>: The antimicrobial activity of the hydroethanolic extracts prepared from 30 plant species was determined against <i>C. acnes</i> standard strains (<i>C. acnes</i> Scholz and Kilian ATCC 11827 and ATCC 11828) and 30 clinical isolates in our preliminary screening. Since acne is an inflammatory skin disease, the anti-inflammatory effect of six active extracts against <i>C. acnes</i> was determined through the in vitro inhibition of collagenase, lipoxygenase (LOX), hyaluronidase and xanthine oxidase (XO) enzymes. <b>Results</b>: <i>Cotinus coggygria</i> Scop. leaf extract displayed the highest hyaluronidase and collagenase inhibition (79.75% and 52.52%, respectively), while the extract from the aerial parts of <i>Helichrysum arenarium</i> (L.) Moench demonstrated a potent XO inhibitory effect (82.51%). Therefore, these two extracts have been chosen for further studies, and LC/MS-MS was used to determine the phenolic profiles of these extracts. <b>Conclusions</b>: Subsequently, nanoemulgels were formulated with the active extracts to develop a prototype herbal anti-acne product, and characterization studies of the formulations were conducted.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 3","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11944516/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143720993","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}