Advances in Pharmacological and Pharmaceutical Sciences最新文献

{"title":"Spray-Dried Powders of Casein-Encapsulated Rutin Stabilized With Sugars for the Enhancement of Intestinal Drug Solubility.","authors":"Helmy Yusuf, Sinta Choirunissa Fitriana, Ni Luh Eradeasty Putri Darmawan, Revalida Ainun Nisa, Retno Sari, Dwi Setyawan","doi":"10.1155/adpp/9952737","DOIUrl":"https://doi.org/10.1155/adpp/9952737","url":null,"abstract":"<p><p>Numerous therapeutic potentials of rutin (RUT) including cardioprotective, neuroprotective, and antihypertension activities have attracted many studies to bring it into clinical use. RUT is phytochemically derived from plants such as apples and tea. It is poorly soluble and very sensible to acidic pH in the stomach environment which leads to conceded oral bioavailability. In contrast, RUT is better soluble in basic environment, thus, encapsulating RUT within enteric microparticles (RUT-MP) using casein (CAS) resolved such problems. The encapsulation by spray-drying employed sugars (lactose, sucrose, and maltodextrin) as bulking agents and for stabilization of the amorphous drug. The developed RUT-MP formulations were prepared in two groups i.e., lower and higher RUT concentrations. The solid states were studied by X-ray diffraction (XRD), differential thermal analysis (DTA) and scanning electron microscopy (SEM). Solubility tests were also carried out on the samples to examine the outcome of the engineered physical modification. The results showed that the RUT-MPs were spherical in morphology. The RUT was transformed into amorphous structure as suggested by the XRD and DTA results indicating that RUT was molecularly dispersed in the RUT-MP. There were no phase separations that occurred as confirmed by the DTA data. Solubility tests carried out on the RUT-MPs showed that the encapsulation with CAS in group with higher concentration of RUT prevented the drug against recovery of the crystallinity and phase separations. The solubility test revealed various substantial enhancements of RUT solubility of the RUT-MPs at pH 7.0. The highest enhancement of RUT solubility was 191,5-fold, with respect to pure RUT. The presence of sugars was beneficial as they improved the yield percentage and might have contributed to the prevention of nano-crystal aggregation which made them a determining aspect for the successful application of spray-dried encapsulation.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2025 ","pages":"9952737"},"PeriodicalIF":2.1,"publicationDate":"2025-03-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11991810/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143952678","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":"Aqueous and Ethanol Extracts of <i>Acacia sieberiana</i> (Fabaceae) Stem Bark Reverse the Pain-Depression Dyad in Mice Through Modulation of Catecholamines, Proinflammatory Cytokines, and Oxidative Stress.","authors":"Sorelle Ngassam Mbankou, Aliance Romain Fokoua, Cedric Wamba Koho, Roger Hermann Sadie Foguieng, Sahar Mofidi Tabatabaei, Pamela Arielle Nono Nankam, Kevin Joseph Tidgewell, Télesphore Benoît Nguelefack","doi":"10.1155/adpp/1244498","DOIUrl":"https://doi.org/10.1155/adpp/1244498","url":null,"abstract":"<p><p><b>Rationale and Objective:</b> The pain-depression dyad is highly prevalent and has reciprocal psychological and behavioral effects, leading to poor quality of life, increased disability, and challenging therapeutic outcomes. In an attempt to find better substances that can target pain-depression comorbidity, we examined the effect of aqueous (AE) and ethanol (EE) extracts from <i>Acacia sieberiana</i> (<i>A. sieberiana</i>) stem bark on reserpinized mice (female and male Swiss albino mice aged 2-3 months). <b>Methods:</b> The dyad was induced with 3 injections (Days 1-3) of reserpine (1 mg/kg/day, <i>s.c</i>.). Then, animals were treated (Days 4-8) with plant extracts (25, 50 and 100 mg/kg/day, <i>p.o</i>.) or L-tryptophane (100 mg/kg/day, <i>i.p</i>.). Pain-like (tactile and cold allodynia) and depression-like (pole, tail suspension, and force swimming tests) behavioral parameters were evaluated on Days 4 and 8. On Day 9, animals were sacrificed for the quantification of acetylcholinesterase activity, oxidative stress parameters, total catecholamines, dopamine, serotonin, IL-1β, and TNF-α levels in the brain or spinal cord. IL-1β and TNF-α were also assayed in the serum. The acute toxicity and phytochemical analysis of EE were conducted. <b>Results:</b> Reserpine-induced tactile and cold allodynia, depression-like behavior, increased serum IL-1β and TNF-α, brain acetylcholinesterase activity, and decreased catecholamine concentration were all reversed by AE and EE. Plant extracts significantly increased dopamine levels and reduced oxidative stress in the brain and/or spinal cord. No significant effect was observed on brain serotonin and TNF-α. EE elicited the best pharmacological activity and was nontoxic. LC-MS/MS molecular networking phytochemical analysis identified 5 compounds with high certainty including piperine, aurantiamide acetate, and asperphenamate. <b>Conclusion:</b> AE and EE are effective against pain and depression. Their pharmacological activities might be related to the modulation of inflammation, oxidative stress and catecholamine, and the presence of bioactive natural products.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2025 ","pages":"1244498"},"PeriodicalIF":2.1,"publicationDate":"2025-02-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11991813/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143959737","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":"Phytochemical Analysis and Pharmaceutical Applications of Monoterpenoids Present in the Essential Oil of <i>Boswellia sacra</i> (Omani Luban).","authors":"Foziya Khan, Luay Rashan","doi":"10.1155/adpp/3536898","DOIUrl":"10.1155/adpp/3536898","url":null,"abstract":"<p><p>Due to its intricacy and long-term usefulness, traditional medicine continues to be practiced in several nations. Among the many medicinal plants found in the Dhofar region of Oman, the aromatic oleo-gum resin generated by <i>Boswellia sacra</i>, commonly referred to as frankincense, stands out for its medical and commercial significance. Resin-carrying ducts are unique to members of the <i>Boswellia</i> family. <i>Boswellia sacra</i> Flueck is one of the 29 species in the genus <i>Boswellia</i> (Burseraceae) and has long been cultivated for its aromatic gums and resins for use as incense. In addition to the resins (60%-80% alcohol soluble), gums (15%-20% water soluble), and essential oil (5%-7%), other components, including polysaccharides and polymeric compounds, also exist in smaller amounts. Physiochemical analyses indicate that <i>Boswellia</i> resin oil is made up of 42.5% diterpenes, 13.1% monoterpenes, and 1% sesquiterpenes. Traditional medicine makes extensive use of frankincense for the treatment of stomach diseases, Alzheimer's disease, and hepatic illnesses. The bioactive chemicals present in frankincense, particularly boswellic acids, are plentiful. The current review examines various compounds present in different species of <i>Boswellia</i>, especially <i>Boswellia sacra</i>, along with their structure.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2025 ","pages":"3536898"},"PeriodicalIF":2.1,"publicationDate":"2025-02-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11876528/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143555599","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":"Pharmaceutical Insights Into Ammi and Parsley: Evaluating Antioxidant Activity, Total Phenolic Content, and Kidney Stone Disintegration Properties.","authors":"Ruba Malkawi, Khairat Battah, Mohammad Alkhreisat","doi":"10.1155/adpp/5522905","DOIUrl":"10.1155/adpp/5522905","url":null,"abstract":"<p><p>This study investigated the pharmaceutical potential of extracts from <i>Ammi visnaga</i> (Ammi) and <i>Petroselinum crispum</i> (Parsley), specifically focusing on their antioxidant activity, total phenolic content, and efficacy in disintegrating calcium oxalate kidney stones. Ammi and Parsley extracts, known for their traditional medicinal uses, contain bioactive compounds with significant antioxidant properties that have attracted attention in pharmaceutical research. Oxidative stress, a key factor in various physiological disorders, underscores the importance of antioxidants in the mitigation of cellular damage. Our investigation revealed concentration-dependent enhancements in antioxidant activity and total phenolic content in both Ammi and Parsley extracts, indicating their potential as natural antioxidant agents. Furthermore, both extracts were effective in reducing the size of calcium oxalate stones, with the Ammi extract demonstrating superior stone-disintegration properties. Dissolution studies have provided valuable insights into the release kinetics of phenolic compounds and antioxidant activity, suggesting sustained therapeutic potential. Overall, Ammi and Parsley extracts show promise in pharmaceutical development, offering alternative therapeutic avenues for managing oxidative stress-related conditions and kidney stone formation.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2025 ","pages":"5522905"},"PeriodicalIF":2.1,"publicationDate":"2025-02-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11867721/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143522140","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":"Phytochemical Composition of <i>Ziziphus lotus</i> (L.) Lam and Its Impact on the Metabolic Syndrome: A Review.","authors":"Chaimae Alla, Amanat Ali, Afaf Mehiou, Youssra Salhi, Nourelhouda Bouanani, Abdelkhaleq Legssyer, Abderrahim Ziyyat","doi":"10.1155/adpp/8276090","DOIUrl":"10.1155/adpp/8276090","url":null,"abstract":"<p><p>The long-term pathological state known as metabolic syndrome is characterized by hypertension, insulin resistance diabetes, abdominal obesity, and hyperlipidemia. Seeking healthcare strategies with fewer side effects, such as herbal remedies, is preferable in terms of mitigating the negative consequences of synthetic medications. <i>Ziziphus lotus</i> (L.) (Rhamnaceae) or wild jujube, commonly known as \"Sedra,\" is one of the best choices as it contains a variety of phytochemicals and biologically active compounds. Several flavonoids and stilbenes have been recognized as the primary bioactive components in wild jujube, including rutin, hyperin, isoquercitrin, and resveratrol. These polyphenols are pharmacologically active and have broad-spectrum beneficial effects for reducing the risk factors associated with metabolic syndrome. They exhibit antioxidant and anti-inflammatory properties, regulate lipid metabolism, and possess antiobesity, antihypertensive, and antidiabetic characteristics. However, there are certain limitations to their therapeutic application, such as low bioavailability. Various strategies have been proposed to enhance their pharmacokinetic profile and therapeutic potential for future use. The main goal of this review is to explore the underlying mechanisms related to the therapeutic effects of wild jujube and its active compounds in the treatment and prevention of metabolic syndrome.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2025 ","pages":"8276090"},"PeriodicalIF":2.1,"publicationDate":"2025-02-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11873318/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143539813","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":"Development of Curcumin Encapsulated Liposomes in Chlorhexidine-Loaded Organogel Using Ternary Phase Systems for Treatment of Omphalitis in Infants.","authors":"Ibilola Mary Cardoso-Daodu, Margaret Okonawan Ilomuanya","doi":"10.1155/adpp/6828052","DOIUrl":"10.1155/adpp/6828052","url":null,"abstract":"<p><p>Infections in infants, after childbirth, remain a leading cause of neonatal morbidity and mortality, globally. A soaring percentage of these infections arise from bacterial colonization of the umbilicus. Current therapy for omphalitis includes the topical application of chlorhexidine on the umbilicus. Bacteria such as <i>Pseudomonas aeruginosa, Escherichia coli, and Staphylococcus aureus,</i> which are the key causative organisms of omphalitis, are resistant to chlorhexidine. In this study, curcumin-loaded liposomes were prepared using the \"thin film hydration\" method. Liposomes were characterized by particle size analysis, light microscopy, encapsulation efficiency, and flux. Stable organogels were formed via a high-speed homogenization method and stabilized by an emulsifier mix. They were evaluated for stability over a period by observing for phase separation. Four gels F1 (curcumin-loaded liposomes in chlorhexidine organogel), F2 (curcumin-loaded liposomes in organogel), F3 (chlorhexidine in organogel), and control (plain organogel) were prepared. Physicochemical properties of all gels were evaluated such as organoleptic tests, gel-to-sol transition, rheological studies, pH, skin irritancy, spreadability, accelerated stability, and antibacterial activity studies. Liposomes were spherical with an average size of 7 μm and an encapsulation efficiency of 97%. The <i>in vitro</i> release profile best fits the Higuchi mathematical model implying that curcumin release was by diffusion and dissolution mechanism. <i>In vitro</i> release was also higher at pH 5.5. F1 had the highest spreadability of 63 mm²g^-1 and the lowest viscosity of 184,400 MPas at a shear rate of 10 rotations per minute with a pH of 6.5. Formulation F1 also displayed the highest antibacterial activity against all three bacteria. It can be concluded that the synergistic interaction between curcumin and chlorhexidine may be responsible for the significant antibacterial potency exhibited in formulation F1. Curcumin-loaded liposomes in chlorhexidine organogel (F1) can serve as a prototype for the development of an antibacterial topical formulation having intrinsic activity and enhanced potency to combat omphalitis.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2025 ","pages":"6828052"},"PeriodicalIF":2.1,"publicationDate":"2025-01-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11824790/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143412979","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":"Insights Into Genetic Variations of the <i>OCT1</i> Gene in Metformin Poor Responders Among Bangladeshi Type 2 Diabetic Patients.","authors":"Rokeya Begum, Arindita Das, Md Jahangir Alam, Gazi Nurun Nahar Sultana","doi":"10.1155/adpp/8568658","DOIUrl":"10.1155/adpp/8568658","url":null,"abstract":"<p><p>Metformin is the most widely prescribed drug for the treatment of Type 2 diabetes mellitus (T2DM), but its response varies from person to person. This study aims to analyze the complete mutation spectrum of the <i>OCT1</i> gene in metformin poor responders and to explore the potential pathogenic effects of the identified mutations. Clinical features of 56 Bangladeshi T2DM patients (who showed altered response to metformin) were analyzed, and genomic DNA was extracted from their blood samples. Subsequently, the entire exons (1-11), along with flanking introns of the <i>OCT1</i> gene were amplified and sequenced. Molecular consequences of the identified mutations on OCT1 protein activity were determined through in silico analyses. In this study, 29 mutations of the <i>OCT1</i> gene were identified; among which 5 mutations (c.412-86G>T, c.970G>C, c.1386-3088_1386-3083delGAATCA, c.1498+66G>T, and c.1653C>A) were novel. It was found that nsSNPs c.181C>T, c.1022C>T, c.493G>T, c.1207A>G, and c.970G>C (novel) as well as frameshift deletions have potential deleterious effects on OCT1 protein stability and function. Some of these mutations also cause alternative splicing, as per the HSF tool. In addition, alteration of interatomic bonding in the OCT1 protein due to two high-risk mutations (c.181C>T and c.1022C>T) was found from web-based analysis. The mutations, as mentioned earlier, are the most probable causative factor of decreased metformin effectiveness and adverse side effects in T2DM patients who are poor responders. Understanding the <i>OCT1</i> gene variations of patients can help tailor treatment strategies for optimal metformin response or identify alternative medications.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2025 ","pages":"8568658"},"PeriodicalIF":2.1,"publicationDate":"2025-01-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11824854/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143412984","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>Sargassum plagiophyllum</i> Ethanolic Extract Enhances Wound Healing by Modulating FAK/Src/Akt/p38 and Rac1 Signaling in Keratinocytes HaCaT Cells.","authors":"Furoida Moolsup, Wanida Sukketsiri, Wipawadee Sianglum, Jirawat Saetan, Nattakanwadee Khumpirapang, Supita Tanasawet","doi":"10.1155/adpp/7198281","DOIUrl":"10.1155/adpp/7198281","url":null,"abstract":"<p><p>Recently, seaweed extracts have been found to have potential in skin benefits. This study, therefore, aimed to explore phytochemical analysis, antimicrobial, antioxidant, and wound healing properties of brown seaweed <i>Sargassum plagiophyllym</i> ethanolic extract (SPEE) on human skin keratinocyte HaCaT cells and the possible mechanism involved. Our results indicated that SPEE contained flavonoid, phenolic, and carotenoid as the major active constituents. The HPLC chromatogram revealed C-phycocyanin and fucoidan presented in SPEE. SPEE demonstrated the antioxidant capability and significantly reduced wound space at 24 and 48 h in wound-healing assay. Treatment with SPEE (50 and 100 μg/mL) increased FAK and Src phosphorylation in western blotting. Moreover, SPEE also upregulated Akt and p38 MAPK phosphorylation but not ERK1/2. SPEE increased Rac1 protein expression. Interestingly, hyaluronan synthase (HAS1 and HAS2) as well as collagen type I and elastin were also significantly upregulated when compared with the control upon exposure to SPEE. In conclusion, our data suggested that SPEE promotes cutaneous wound healing by regulating FAK/Src-mediated Akt, p38 MAPK, and Rac1 signaling. These findings suggest the potential use of SPEE for skin wound treatment.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2025 ","pages":"7198281"},"PeriodicalIF":2.1,"publicationDate":"2025-01-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11779993/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143063222","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":"Method Development and Clinical Utility for Simultaneous Measurement of 21-Deoxycortisol, 17-Hydroxyprogesterone, Cortisol, and Cortisone Levels in Human Plasma Using UHPLC-MS/MS.","authors":"Syed N Alvi, Saleh Al Dgither, Ali Al-Odaib","doi":"10.1155/adpp/3859670","DOIUrl":"10.1155/adpp/3859670","url":null,"abstract":"<p><p>A simple and efficient validated assay for quantifying 21-deoxycortisol (21-DOC), 17-hydroxyprogesterone (17-OHP), cortisol, and cortisone in human plasma has been developed using ultra-high performance liquid chromatography coupled with tandem mass spectrometry (UHPLC-MS/MS). Analysis of plasma samples were performed on Atlantis dC18 (3 <i>μ</i>m) column using a mobile phase of 20.0 mM ammonium acetate and acetonitrile (50:50, <i>v</i> : <i>v</i>) that was delivered at isocratic flow rate 0.3 mL/minute. After addition of d4-cortisol as an internal standard (IS), plasma samples containing 21-DOC, 17-OHP, cortisol, and cortisone were extracted with mixture of dichloromethane and tert-butylmethyl ether 1:2 (<i>v</i>/<i>v</i>). Analytes were detected and quantified in the positive ion mode of electrospray ionization using multiple reaction monitoring transition set at mass to charge (m/z): 347.17 ⟶ 311.12, 331.17 ⟶ 96.97, 363.11 ⟶ 121.00, 361.18 ⟶ 163.11, and 367.19 ⟶ 121.24 for 21-DOC and 17-OHP, cortisol, cortisone, and cortisol-d4 (IS), respectively. The relationship between concentration and peak area response (analyte/IS) were linear over the range of 0.25-50, 0.5-100, 1-200, and 2-400 ng/mL for 21-DOC, 17-OHP, cortisone, and cortisol, respectively. The mean extraction recovery of the analytes was in the range of 83%-96%. The coefficient of variation within and between days was less than 13.6%, and the bias ranged from -9.2% to 12%. The measured level of cortisol, cortisone, and 17-OHP was in the range of 21.9-110, 4.33-12.71, and 0.37-1.4 ng/mL, respectively. Furthermore, the measured value of cortisone-cortisol ratio was in the range of 0.08-0.21.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2025 ","pages":"3859670"},"PeriodicalIF":2.1,"publicationDate":"2025-01-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11759567/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143045451","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":"Formulation Design, Optimization, and Evaluation of Solid Lipid Nanoparticles Loaded With an Antiviral Drug Tenofovir Using Box-Behnken Design for Boosting Oral Bioavailability.","authors":"Sri Rekha M, Sangeetha S","doi":"10.1155/2024/5248746","DOIUrl":"https://doi.org/10.1155/2024/5248746","url":null,"abstract":"<p><p><b>Purpose:</b> The current study aimed to improve the oral bioavailability of tenofovir (TNF), an antihuman immunodeficiency viral (HIV) drug, by integrating it into solid lipid nanoparticles (SLNs), an emerging lipid formulation. <b>Method:</b> The suggested SLNs were generated utilizing the microemulsion process, using Compritol 888 ATO. A Box-Behnken experimental design was attempted to analyze the impact of critical quality attributes (CQAs), such as lipid and surfactant content and homogenization duration on response metrics such as particle size (PS) and percentage entrapment. The prepared SLNs were assessed for entrapment efficiency, zeta potential (ZP), PS, polydispersity index, and in vitro drug release. Moreover, ex vivo permeation tests employing goat intestinal sacs, solid-state characterization by DSC and PXRD, surface morphology by SEM, and in vivo pharmacokinetic evaluation using albino Wistar rats were conducted. <b>Results:</b> The research findings demonstrated that a formulation composed of 5.5% lipid and 2% surfactant had a comparatively smaller PS (449.90 ± 4.79 nm), a narrow size distribution (0.304 ± 0.004), and strong stability with an entrapment efficiency of 83.13 ± 6.34% and a negative ZP (-18.10 ± 2.35 mV). According to in vitro drug release experiments, first-order kinetics were followed and 99% of the medication was released over the time course of 24 h. In albino Wistar rats, an in vivo pharmacokinetic analysis of the optimized formulation (F10) showed a 12.4-fold improvement in bioavailability over pure TNF solution. <b>Conclusion:</b> This study suggests the potential of SLNs in overcoming bioavailability issues, particularly low permeability, gut metabolism, and P-gp efflux transport.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2024 ","pages":"5248746"},"PeriodicalIF":2.1,"publicationDate":"2024-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11707065/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142942535","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}