ADMET and DMPK最新文献

{"title":"Molecular properties, including chameleonicity, as essential tools for designing the next generation of oral beyond rule of five drugs.","authors":"Diego García Jiménez, Maura Vallaro, Luigi Vitagliano, Lucía López López, Giulia Apprato, Giuseppe Ermondi, Giulia Caron","doi":"10.5599/admet.2334","DOIUrl":"https://doi.org/10.5599/admet.2334","url":null,"abstract":"<p><strong>Background and purpose: </strong>The classical drug discovery toolbox continually expands beyond traditional rule of five (Ro5)-compliant small molecules to include new chemical modalities for difficult-to-drug targets. The paper focuses on the molecular properties essential to drive oral bioavailability within the bRo5 framework.</p><p><strong>Experimental approach: </strong>The first part outlines the concept and methodologies for characterizing bRo5 physicochemical properties, including considerations on chameleonicity; in particular, the paper summarizes the content of the last author's talk presented during the IAPC-10 Meeting held in Belgrade in September 2023 (https://iapchem.org/index.php/iapc-10-home). The second part of the manuscript presents novel experimental and computational data on three proteolysis targeting chimeras (PROTACs) currently in clinical trials.</p><p><strong>Key results: </strong>Molecular descriptors of ARV-110, ARV-471, and DT-2216 are reported and the main limitations of the applied experimental approaches are discussed. Moreover, a simple computational method shows how predicting the presence of chameleonic effects.</p><p><strong>Conclusion: </strong>A full complete physicochemical characterization of three degraders in clinical trials is reported to highlight the differences in physicochemical descriptors between PROTACs dosed orally and intravenously.</p>","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"12 5","pages":"721-736"},"PeriodicalIF":3.4,"publicationDate":"2024-08-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11542721/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142612104","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Cerium oxide nanoparticles-assisted aptasensor for chronic myeloid leukaemia detection.","authors":"Yuspian Nur, Muhammad Ihda Hl Zein, Irkham Irkham, Shabarni Gaffar, Toto Subroto, Yeni Wahyuni Hartati","doi":"10.5599/admet.2404","DOIUrl":"https://doi.org/10.5599/admet.2404","url":null,"abstract":"<p><strong>Background and purpose: </strong>Chronic myeloid leukaemia (CML) is one of the most lethal types of leukaemia and can rapidly progress if not treated properly. Therefore, having an effective diagnostic strategy is crucial. Various methods are available for diagnosis, including electrochemical biosensors with aptamer bioreceptors.</p><p><strong>Experimental approach: </strong>In this study, we immobilized the KK1D04 aptamer on a screen-printed carbon electrode (SPCE) supported by CeO₂ nanoparticles (CeO₂NPs) to detect K562 cells, a type of CML cell line. Several parameters were optimized to enhance the aptasensor response using the Box-Behnken experimental design.</p><p><strong>Key results: </strong>The developed aptasensor demonstrated good performance with a limit of detection (LOD) and limit of quantification (LOQ) of 16 cells/mL and 3,882 cells/mL, respectively, in the K562 cell concentration range of 10² to 10⁶ cells/mL. The optimum experimental conditions were an aptamer concentration of 0.8 ppm, an aptamer incubation time of 36 minutes, and a K562 aptamer-cell incubation time of 13 minutes. The aptasensor also exhibits selectivity for K562 cells compared to Vero cells, THP1 cells, and Raji cells.</p><p><strong>Conclusion: </strong>The aptasensor in this study demonstrated the potential to detect K562 cells. These results could contribute to the advancement of point-of-care (POC) devices for the detection of CML.</p>","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"12 4","pages":"623-635"},"PeriodicalIF":3.4,"publicationDate":"2024-08-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11517519/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142543042","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"<i>Ex vivo</i> propofol permeation across nasal mucosa: A proof-of-concept study for outpatient light sedation via nasal route.","authors":"Michele D Spampinato, Anna Costanzini, Roberto De Giorgio, Angelina Passaro, Nicola Realdon, Fabrizio Bortolotti, Sabrina Banella, Gaia Colombo","doi":"10.5599/admet.2403","DOIUrl":"https://doi.org/10.5599/admet.2403","url":null,"abstract":"<p><strong>Background and purpose: </strong>Aiming to achieve light sedation via intranasal administration, this study showed that propofol (PPF) did not permeate across the rabbit nasal mucosa ex vivo from its marketed emulsion for injection.</p><p><strong>Experimental approach: </strong>Dilution of the emulsion with methyl-β-cyclodextrin in saline solution increased propofol solubility in water and diffusion across the nasal epithelium.</p><p><strong>Key results and conclusion: </strong>Despite these positive effects of the cyclodextrin, the amount of PPF permeated was minimal in 3 h, exceeding the formulation residence time in the nose. These results highlight the key role of formulation and the need for innovation in solubility and transmucosal transport enhancement techniques to optimize drug delivery and therapeutic efficacy.</p>","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"12 5","pages":"759-768"},"PeriodicalIF":3.4,"publicationDate":"2024-08-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11542715/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142612097","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The biological applications of IPN hydrogels.","authors":"María I León-Campos, Juan J Mendoza, Hilda Aguayo-Morales, Luis E Cobos-Puc, Denis A Cabrera-Munguía, Jesús A Claudio-Rizo","doi":"10.5599/admet.2398","DOIUrl":"https://doi.org/10.5599/admet.2398","url":null,"abstract":"<p><strong>Background and purpose: </strong>Interpenetrating polymer network (IPN) hydrogels are an adaptable category of materials, exhibiting remarkable promise for various biological applications due to their distinctive structural and functional attributes. This review delves into the synthesis of IPN hydrogels through both physical and chemical methodologies, elucidating how these techniques allow for precise tailoring of mechanical properties, swelling behaviour, and biocompatibility.</p><p><strong>Experimental approach: </strong>We conducted an extensive literature review by searching well-established online research databases for articles published since 2009 to gather comprehensive data on IPN hydrogels.</p><p><strong>Key results: </strong>Our review highlights several critical applications of IPN hydrogels in the biomedical field; i) Tissue engineering: IPN hydrogels are evaluated for their capacity to emulate the extracellular matrix, making them excellent scaffolds for tissue engineering; ii) Controlled drug release: The ability of IPN hydrogels to modulate drug release rates and protect bioactive molecules is explored. Their structure enables sustained and targeted delivery of therapeutic agents, enhancing treatment efficacy; iii) 3D bioprinting: The use of IPN hydrogels as bioinks for 3D bioprinting is assessed, demonstrating their capability to construct intricate, biomimetic structures with high precision; and iv) Regenerative medicine: the development of biomimetic IPN hydrogels for regenerative medicine, emphasizing their potential to closely replicate natural biological environments, thereby promoting effective tissue repair and regeneration.</p><p><strong>Conclusion: </strong>IPN hydrogels emerge as a versatile and multifaceted platform with significant implications for advancing biomedical science and clinical therapies. Their diverse applications highlight their potential to revolutionize current biomedical practices and contribute to the development of innovative therapeutic solutions.</p>","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"12 4","pages":"581-621"},"PeriodicalIF":3.4,"publicationDate":"2024-08-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11517517/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142543046","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Analgesic effects of intraarticular anaesthetic lidocaine and methylprednisolone versus methylprednisolone alone following knee arthroscopy.","authors":"Wahid Mohammed Hassan, Anas Amer Mohammad","doi":"10.5599/admet.2412","DOIUrl":"https://doi.org/10.5599/admet.2412","url":null,"abstract":"<p><strong>Background: </strong>Knee arthroscopy is a widely practiced orthopaedic procedure known for its minimally invasive approach, allowing quicker recovery times and less postoperative discomfort than traditional open surgeries. However, managing postoperative pain remains a critical aspect of patient care and satisfaction. The main objective of this research is to examine the relationships between patient demographics (age, gender, BMI) and early postoperative outcomes, including pain, physiotherapy, and walking.</p><p><strong>Method: </strong>Randomized data collection, clinical trial study of 2 groups of patients. The patients were split into lidocaine 1 % 16 ml + methylprednisolone 160 mg 4 ml) and (methylprednisolone only 160 mg 4 ml) groups. All patients in both groups were queried about age, gender, BMI, and pain on the first, third, and 15th days following surgery. All patients were tested for physiotherapy on the second, third, and fourth postop days. After surgery, walking was tested on the third, fourth, and fifth days.</p><p><strong>Results: </strong>Significant differences in postoperative pain relief and physiotherapy initiation times were observed. There are notable associations between treatment groups and recovery metrics, such as pain levels and mobility on various days' post-surgery. Significant demographic influences (age, gender, BMI) on recovery outcomes are observed, particularly in walking and pain at day 15 post-operation.</p><p><strong>Conclusion: </strong>lidocaine and methylprednisolone improve postoperative pain relief and functional recovery in knee arthroscopy patients, with most experiencing reduced pain early post-surgery (early physiotherapy) and an expedited return to walking (decreased morbidity). Patients taking just methylprednisolone recovered slower. Age, gender, and BMI affected pain and walking abilities post-operation but not physiotherapy time, underscoring the personalised approach needed in postoperative treatment.</p>","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"12 4","pages":"679-685"},"PeriodicalIF":3.4,"publicationDate":"2024-08-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11517516/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142543041","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Optimizing gefitinib nanoliposomes by Box-Behnken design and coating with chitosan: A sequential approach for enhanced drug delivery.","authors":"Seema Rohilla, Rajendra Awasthi, Ankur Rohilla, Sachin Kumar Singh, Dinesh Kumar Chellappan, Kamal Dua, Harish Dureja","doi":"10.5599/admet.2366","DOIUrl":"https://doi.org/10.5599/admet.2366","url":null,"abstract":"<p><strong>Background and purpose: </strong>This study aimed to improve the stability and prolonged gefitinib release from the nanoliposomes.</p><p><strong>Experimental approach: </strong>Nanoliposomes were prepared by reverse-phase evaporation and optimized using Box-Behnken design to investigate the influence of sonication time (<i>X</i> ₁), tween 80 / soya phosphatidylcholine ratio (<i>X</i> ₂), and cholesterol/soya phosphatidylcholine ratio (<i>X</i> ₃) on nanoliposomes.</p><p><strong>Key results: </strong>Optimized nanoliposomes were quasi-spherical shaped, with a mean dimension of 93.2 nm and an encapsulation efficiency of 87.56±0.17 %. Surface decoration of the optimized batch was done using different concentrations of chitosan. The optimal chitosan concentration required to adorn the nanoliposome surface was 0.01 %. In comparison to unadorned nanoliposomes (82.16±0.65 %), adorned nanoliposomes (78.04±0.35 %) released the drug consistently over 24 h via Fickian diffusion. The IC₅₀ values for surface-adorned nanoliposomes in A549 and H1299 cells were 6.53±0.75 and 4.73±0.46 μM, respectively. Cytotoxicity of the surface-decorated nanoliposomes may be due to their higher zeta potential and prolonged drug release. At the end of the sixth month, the samples stored at 4 °C were more stable than those stored at 25 °C and 45 °C. The stability of plain nanoliposomes has increased after chitosan coating. Thus, by using different concentrations of chitosan solution as coating material, we can develop a suitable sustained drug-release surface-adorned nanoliposomal formulation.</p><p><strong>Conclusion: </strong>The developed nanoliposomes may offer a new path for melanoma clinics.</p>","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"12 4","pages":"657-677"},"PeriodicalIF":3.4,"publicationDate":"2024-07-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11517515/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142543045","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Impact of lactoferrin supplementation on cotrimoxazole pharmacokinetics: A preliminary clinical investigation.","authors":"Dion Notario, Angela Marietha Munzir, Yulina Novella, Linawati Hananta","doi":"10.5599/admet.2358","DOIUrl":"10.5599/admet.2358","url":null,"abstract":"<p><strong>Background and purpose: </strong>Cotrimoxazole, a commonly prescribed antibiotic, has substantial resistance, especially in Indonesia, with its uropathogenic resistance reaching 67% in 2017. Although cotrimoxazole has been suggested to be co-administered with lactoferrin to enhance its antibacterial effectiveness and this practice has been widely adopted since the Covid-19 pandemic, the impact of lactoferrin on the pharmacokinetics of cotrimoxazole remains relatively unknown. This study aims to conduct a preliminary clinical investigation into the impact of lactoferrin supplementation on the pharmacokinetics of cotrimoxazole, focusing on the elimination rate and excretion of unchanged drug in urine.</p><p><strong>Experimental approach: </strong>This study employed a blinded, cross-over, single-dose pharmacokinetics investigation, which included five healthy volunteers as participants. In the initial period, the first group received cotrimoxazole (80 mg trimethoprim and 400 mg sulfamethoxazole) along with a lactoferrin-containing supplement, while the second group only received cotrimoxazole. Subsequently, after a washout period, the conditions were reversed. Urine sampling was conducted at intervals from 0 to 24 hours post-medication, and drug levels in the urine were determined using high-performance liquid chromatography.</p><p><strong>Key results: </strong>The population-based pharmacokinetic analysis revealed that the optimal model was the one-compartment model with first-order elimination and proportional residual error.</p><p><strong>Conclusion: </strong>The findings show that the administration of lactoferrin-containing supplements did not significantly influence the covariate model and, therefore, did not alter the pharmacokinetics parameter of cotrimoxazole in urine with a single administration, implying that lactoferrin did not cause drug interaction problems when given simultaneously.</p>","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"12 3","pages":"543-551"},"PeriodicalIF":3.4,"publicationDate":"2024-06-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11289514/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141873928","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Fast and simple voltammetric sensing of avanafil in the pharmaceutical formulation by using unmodified boron-doped diamond electrode.","authors":"Hoshyar Saadi Ali, Hemn A H Barzani, Yavuz Yardım","doi":"10.5599/admet.2357","DOIUrl":"10.5599/admet.2357","url":null,"abstract":"<p><strong>Background and purpose: </strong>Erectile dysfunction is a common issue among adult males involving difficulty in maintaining an erection, and it is often treated with fast-acting, low-side-effect drugs like avanafil (AVN), among other phosphodiesterase-5 inhibitors. Hence, developing fast, simple, and sensitive methods to detect AVN is crucial.</p><p><strong>Experimental approach: </strong>This study conducts an electroanalytical inquiry and provides a new voltammetric method for accurately analyzing AVN utilizing a boron-doped diamond (BDD) electrode without any modifications.</p><p><strong>Key results: </strong>In the Britton-Robinson buffer (BR, 0.04 mol L^-1, pH 4.0), cyclic voltammetry showed a clearly defined and irreversible anodic peak at around +1.44 V relative to Ag/AgCl. The pH of the solution was shown to have an impact on the voltammetric signals of the oxidation peaks. A good linear response for AVN quantification was achieved using square-wave voltammetry. This was done in a 0.04 mol L-1 BR (pH 4.0) solution at a potential of +1.33 V (<i>vs.</i> Ag/AgCl). The method exhibited a wide dynamic range of 0.5 to 30.0 μg mL^-1 (1.0 to 62 μmol L^-1) and a low limit of detection of 0.14 μg mL^-1 (0.29 μmol L^-1). The method proposed demonstrated suitability for determining AVN content in pharmaceutical formulations. The accuracy of the approach was demonstrated by comparing the results obtained using the developed method with those achieved using the UV-Vis spectrometry method.</p><p><strong>Conclusion: </strong>Our method simplifies the analytical process by eliminating the need for electrode modification, reducing both time and resource requirements while enhancing overall feasibility.</p>","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"12 3","pages":"529-542"},"PeriodicalIF":3.4,"publicationDate":"2024-06-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11289509/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141873927","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Berberine HCl and diacerein loaded dual delivery transferosomes: Formulation and optimization using Box-Behnken design.","authors":"Siddharth Singh, Rajendra Awasthi","doi":"10.5599/admet.2268","DOIUrl":"10.5599/admet.2268","url":null,"abstract":"<p><strong>Introduction: </strong>Berberine is a poorly water-soluble alkaloid compound showing significant anti-inflammatory characteristics. It reduces the levels of pro-inflammatory and inflammatory cytokines, including tumour necrosis factor (TNF-α, IFN-γ) and interleukin (IL-23, IL-12, and IL-23). Diacerein significantly reduces the splenomegaly associated with psoriasis. It downregulates the production of TNF-α and IL-12.</p><p><strong>Method: </strong>This study reported the development of transferosomes containing berberine HCl and diacerein using a film hydration method followed by optimization using a Box-Behnken design. Sodium deoxycholate was used as an edge activator. The impact of independent variables (amount of phosphatidylcholine, amount of edge activator, and sonication cycles) on dependent variables (particle size and entrapment efficiency) was examined. The optimized formulation was characterized for polydispersity index, vesicle size, entrapment efficiency, ζ potential, spectral analysis like Fourier transform infrared, thermal analysis, X-ray diffraction, deformability, transmission electron microscopy, antioxidant assay, <i>in-vitro</i> release, and <i>ex-vivo</i> skin permeation studies.</p><p><strong>Results: </strong>The optimized formulation had a particle size of 110.90±2.8 nm with high entrapment efficiency (89.50±1.5 of berberine HCl and 91.23±1.8 of diacerein). Deformability, polydispersity index, ζ potential, and antioxidant activity of the optimized formulation were 2.44, 0.296, -13.3, and 38.36 %, respectively. Optimized transferosomes exhibited 82.093±0.81 % and 85.02±3.81 % release of berberine HCl and diacerein after 24 h of dissolution study. The transdermal flux of optimized formulation was 0.0224 μg cm^-2 h^-1 (2.24 cm h^-1 permeation coefficient) and 0.0462 μg cm^-2 h^-1 (4.62 cm h^-1 permeation coefficient), respectively, for berberine HCl and diacerein. Raman analysis of treated pig skin confirmed that the transferosomes can permeate the skin. No change in the skin condition or irritation was observed in BALB/c mice. Formulation stored at 4 and 25±2 °C / 60±5 % relative humidity was stable for 3 months.</p><p><strong>Conclusions: </strong>Thus, the results demonstrated successful optimization of the transferosomes for the efficient topical delivery of berberine HCl and diacerein in the effective management of psoriasis.</p>","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"12 3","pages":"553-580"},"PeriodicalIF":3.4,"publicationDate":"2024-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11289510/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141873926","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Propolis-loaded liposomes: characterization and evaluation of the <i>in vitro</i> bioaccessibility of phenolic compounds.","authors":"Oznur Saroglu, Ayse Karadag","doi":"10.5599/admet.2204","DOIUrl":"10.5599/admet.2204","url":null,"abstract":"<p><strong>Background and purpose: </strong>Propolis has low water solubility, poor stability, and limited bioaccessibility of phenolic constituents when subjected to <i>in vitro</i> digestion. To overcome these drawbacks, the liposomal encapsulation method can be employed.</p><p><strong>Experimental approach: </strong>Soybean phosphatidylcholine lecithin mixed with Tween 80 (T80) and ammonium phosphatides (AMP) was used to produce propolis extract (PE)-loaded liposomes. The mean particle size, zeta potential, encapsulation efficiency values, and transmission electron microscopy analysis were used to characterize liposomes. Individual phenolics were determined for digested and nondigested propolis-loaded liposomes and propolis extract.</p><p><strong>Key results: </strong>Tween 80 incorporation reduced the size of unloaded liposomes, whereas AMP inclusion yielded larger liposomes. In both formulations, PE loading significantly increased the size and reduced the zeta potential values and homogeneity of the size distribution. In free PE, the most bioaccessible polyphenols were phenolic acids (3.20 to 5.63 %), and flavonoids such as caffeic acid phenethyl ester, galangin, pinobanksin, and pinocembrin (0.03 to 2.12 %) were the least bioaccessible. Both liposomal propolis provided significantly higher bioaccessibility of phenolic compounds. The liposomes with T80 and AMP in their compositions recovered 52.43 and 185.90 % of the total amount of phenolic compounds in the nondigested samples, respectively. The liposomes containing AMP not only exhibited high solubility for PE but also provided protection to the phenolic compounds during <i>in vitro</i> digestion.</p><p><strong>Conclusion: </strong>Liposomal encapsulation could be a promising approach to improving the solubility and stability of PE in digestive fluids, making it suitable for the delivery of propolis in oral formulations.</p>","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"12 1","pages":"209-224"},"PeriodicalIF":3.4,"publicationDate":"2024-02-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10974815/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140334302","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}