Drug Development and Industrial Pharmacy最新文献

{"title":"Computer-aided optimization of carbidopa/levodopa orally disintegrating tablets.","authors":"Fucheng Qin, Congcong Wan, Yuanyuan Zhang","doi":"10.1080/03639045.2024.2327475","DOIUrl":"10.1080/03639045.2024.2327475","url":null,"abstract":"<p><strong>Objective: </strong>This study aimed to optimize the formulation of carbidopa/levodopa orally disintegrating tablets (ODTs) in order to improve their disintegration performance, and facilitate easier medication intake for Parkinson's patients.</p><p><strong>Method: </strong>The response surface methodology (RSM) was used to optimize the formulation, with the content of cross-linked polyvinylpyrrolidone (PVPP), microcrystalline cellulose (MCC), and mannitol (MNT) as independent variables, and disintegration time as the response parameter. Python was utilized to model Carr Indices and mixing time to determine the suitable mixing time. Direct compression (DC) was used for the preparation of ODTs.</p><p><strong>Result: </strong>The optimization process resulted in the following values for the independent variables: 7.04% PVPP, 22.02% MCC, and 16.21% MNT. By optimizing the mixing time using Python, it was reduced to 14.19 min. The ODTs prepared using the optimized formulation and a mixing time of 14.19 min exhibited disintegration times of 16.74 s <i>in vitro</i> and 17.63 s <i>in vivo</i>. The content uniformity of levodopa and carbidopa was found to be 100.83% and 99.48%, respectively.</p><p><strong>Conclusion: </strong>The ODTs optimized using RSM and Python demonstrated excellent disintegration performance, leading to a decrease in the time the drug exists in solid form in the oral cavity. This improvement in disintegration time reduced the difficulty of swallowing for patients and enhanced medication compliance, while still ensuring that ODTs prepared by DC had sufficient mechanical strength to meet storage and transportation requirements.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":null,"pages":null},"PeriodicalIF":3.4,"publicationDate":"2024-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140058918","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Development and characterization of 3D printed ethylene vinyl acetate (EVA) as drug delivery device for the treatment of overactive bladder.","authors":"Gustavo Ferrari, Loise Silveira da Silva, Renata Cerruti, Izabelle de Mello Gindri, Gean Vitor Salmoria, Carlos Rodrigo de Mello Roesler","doi":"10.1080/03639045.2024.2311177","DOIUrl":"10.1080/03639045.2024.2311177","url":null,"abstract":"<p><p>The overactive bladder is a condition characterized by a sudden urge to urinate, even with small volumes of urine present in the bladder. The current treatments available for this pathology consist on conservative approaches and the continuous administration of drugs, which when made by conventional methods has limitations related to the first pass metabolism, bioavailability, severe side effects, and low patient adherence to treatments, ultimately leading to low effectiveness. Within this context, the present work proposes the design, manufacture, and characterization of an intravesical implant for the treatment of overactive bladder pathology, using EVA copolymer as a matrix and oxybutynin as a drug. The fabrication of devices through two manufacturing techniques (extrusion and additive manufacturing by fused filament fabrication, FFF) and the evaluation of the implants through characterization tests was proposed. The usability and functionality were evaluated through simulated insertion of the device/prototype in a bladder model through catheter insertion tests. The safety and effectiveness of the devices was investigated from mechanical testing as well as drug release assays. Drug release assays presented a burst release in the first 24 h, followed by a release of 1.8 and 2.8 mg/d, totalizing 32 d. Mechanical tests demonstrated an increase in the stiffness of the specimens due to the addition of the drug, showing a change in maximum stress and strain at break. The released dose was higher than that usually presented when considering the oral administration route, showing the optimization of the development of this implant has the potential to improve the quality of life of patients with overactive bladder.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":null,"pages":null},"PeriodicalIF":3.4,"publicationDate":"2024-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140130973","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Combined eutexia and amorphization for simultaneous enhancement of dissolution rate of triamterene and hydrochlorothiazide: preparation of orodispersible tablets.","authors":"Hend A Awad, Mohamed I Fetouh, Amal A Sultan, Gamal M El Maghraby","doi":"10.1080/03639045.2024.2323996","DOIUrl":"10.1080/03639045.2024.2323996","url":null,"abstract":"<p><strong>Background: </strong>Triamterene is an oral antihypertensive drug with dissolution-limited poor bioavailability. It can be used as monotherapy or in fixed dose combination with hydrochlorothiazide which also suffers from poor dissolution. Moreover, co-processing of drugs in fixed dose combination can alter their properties. Accordingly, pre-formulation studies should investigate the effect of co-processing and optimize the dissolution of drugs before and after fixed dose combination. This is expected to avoid deleterious interaction (if any) and to hasten the biopharmaceutical properties.</p><p><strong>Objective: </strong>Accordingly, the aim of this work was to optimize the dissolution rate of triamterene alone and after fixed dose combination with hydrochlorothiazide.</p><p><strong>Methodology: </strong>Triamterene was subjected to dry co-grinding with xylitol, HPMC-E5 or their combination. The effect of co-grinding with hydrochlorothiazide was also tested in absence and presence of xylitol and HPMC-E5. The products were assessed using Fourier-transform infrared (FTIR), differential scanning calorimetry, X-ray powder diffraction (XRPD), in addition to dissolution studies. Optimum formulations were fabricated as oral disintegrating tablets (ODT).<b>Results:</b> Co-processing of triamterene with xylitol formed eutectic system which hastened dissolution rate. HPMC-E5 resulted in partial amorphization and improved triamterene dissolution. Co-grinding with both materials combined their effects. Co-processing of triamterene with hydrochlorothiazide resulted in eutexia but the product was slowly dissolving due to aggregation. This problem was vanished in presence of HPMC-E5 and xylitol. Compression of the optimum formulation into ODT underwent fast disintegration and liberated acceptable amounts of both drugs.</p><p><strong>Conclusion: </strong>The study introduced simple co-processing with traditional excipients for development of ODT of triamterene and hydrochlorothiazide.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":null,"pages":null},"PeriodicalIF":3.4,"publicationDate":"2024-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139943983","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Construction and <i>in vitro</i>/<i>in vivo</i> evaluation of menantine hydrochloride oral liquid sustained-release drug delivery system.","authors":"Hongfei Liu, Ying Bao, Xiangping Lai, Yingshu Feng, Dan Yang, Rui Sun, Caleb Kesse Firempong, Haibing He","doi":"10.1080/03639045.2024.2329746","DOIUrl":"10.1080/03639045.2024.2329746","url":null,"abstract":"<p><strong>Objective: </strong>The purpose of the present study was to formulate a menantine hydrochloride (MH) sustained-release suspension.</p><p><strong>Methods: </strong>Menantine hydrochloride drug resin complex (MH-DRC) was prepared with strong acid cation exchange resin as carrier using water bath method. The MH-DRC was characterized using scanning electron microscopy, X-ray diffraction and infrared spectroscopy. The MH-coated microcapsule (MH-CM) with optimized formulation was further dispersed in a suitable medium to obtain a sustained-release suspension. The rats were given both the MH sustained-release suspension and the commercial MH sustained-release capsule by intragastric administration. The plasma concentration-time curves and related pharmacokinetic parameters were also investigated using a non-atrioventricular model.</p><p><strong>Results: </strong>MH and ion-exchange resin were ionically bonded. AmberliteIRP®69 had a higher affinity for MH at the initial concentration of 5 mg·mL^-1 and a reaction temperature of 25.0 ± 0.5 °C. <i>In vitro</i> drug release profile showed that both the drug resin complex and the coated microcapsules had a certain level of sustained-release effect. The <i>t_1/2</i> of MH sustained-release suspension was extended from 68.44 h to 72.79 h with the peak blood concentration being decreased to 3.56 μg·mL^-1 and the <i>T_max</i> extended to 12 h compared with the commercial MH sustained-release capsule. The concentration-time curve of the self-made MH sustained-release suspension was flattened and the average relative bioavailability (<i>F_r</i>) was 116.65% compared with the commercial MH sustained-release capsules.</p><p><strong>Conclusions: </strong>The findings showed that the MH sustained-release suspension was successfully formulated with acceptable pharmacokinetic indices for effective treatment of Alzheimer's disease.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":null,"pages":null},"PeriodicalIF":3.4,"publicationDate":"2024-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140119094","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"<i>In vitro</i> evaluation of physicochemical-dependent effects of polymeric nanoparticles on their cellular uptake and co-localization using pulmonary calu-3 cell lines.","authors":"Nashwa Osman, Paul Curley, Helen Box, Neill Liptrott, Darren Sexton, Imran Saleem","doi":"10.1080/03639045.2024.2332889","DOIUrl":"10.1080/03639045.2024.2332889","url":null,"abstract":"<p><strong>Objective: </strong>The study evaluated physicochemical properties of eight different polymeric nanoparticles (NPs) and their interaction with lung barrier and their suitability for pulmonary drug delivery.</p><p><strong>Methods: </strong>Eight physiochemically different NPs were fabricated from Poly lactic-co-glycolic acid (PLGA, PL) and Poly glycerol adipate-co-ω-pentadecalactone (PGA-co-PDL, PG) <i>via</i> emulsification-solvent evaporation. Pulmonary barrier integrity was investigated <i>in vitro</i> using Calu-3 under air-liquid interface. NPs internalization was investigated using a group of pharmacological inhibitors with subsequent microscopic visual confirmation.</p><p><strong>Results: </strong>Eight NPs were successfully formulated from two polymers using emulsion-solvent evaporation; 200, 500 and 800 nm, negatively-charged and positively-charged. All different NPs did not alter tight junctions and PG NPs showed similar behavior to PL NPs, indicating its suitability for pulmonary drug delivery. Active endocytosis uptake mechanisms with physicochemical dependent manner were observed. In addition, NPs internalization and co-localization with lysosomes were visually confirmed indicating their vesicular transport.</p><p><strong>Conclusion: </strong>PG and PL NPs had shown no or low harmful effects on the barrier integrity, and with effective internalization and vesicular transport, thus, prospectively can be designed for pulmonary delivery applications.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":null,"pages":null},"PeriodicalIF":3.4,"publicationDate":"2024-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140293089","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A newly developed UPLC-MS/MS method for simultaneous quantitative analysis of ajuforrestin A, ajuforrestin B, ajugamacrin and 8-O-acetylharpagide derived from <i>Ajuga</i> plants in mice blood and the <i>in vivo</i> pharmacokinetics.","authors":"Xiuwei Shen, Chen Chen, Congcong Wen, Shuaishuai Yu, Huamin Liu, Xiaomin Gao, Lianguo Chen","doi":"10.1080/03639045.2024.2328731","DOIUrl":"10.1080/03639045.2024.2328731","url":null,"abstract":"<p><strong>Objective: </strong>To develop a sensitive and fast detection method <i>via</i> ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) to assess the concentration of ajuforrestin A, ajuforrestin B, ajugamacrin and 8-O-Acetylharpagide primarily derived from <i>Ajuga</i> plants in mice blood and their pharmacokinetics.</p><p><strong>Methods: </strong>Single protein precipitation with high-proportioned acetonitrile is chosen for sample clean-up. The UPLC HSS T3 (2.1 mm × 100 mm, 1.8 µm) column with a mobile phase in gradient elution mode at the flow rate of 0.4 mL/min was used for sample separation. Acetonitrile was selected as the organic phase solution and water containing 0.1% formic acid was chosen as the aqueous solution. A tandem mass spectrometer containing an electrospray ionization (ESI) source in the positive ionization mode was used to detect four compounds <i>via</i> multiple reaction monitoring (MRM).</p><p><strong>Results: </strong>The calibration curves (5-1000 ng/mL) of four compounds were linear with correlation coefficients > 0.997. The matrix effects, accuracy, precision, and recovery were all within permissible scope.</p><p><strong>Conclusions: </strong>In this approach, the corresponding pharmacokinetic parameters were successfully clarified in mouse for the first time, which provided a theoretical basis for the improvement of the standard of <i>Ajuga</i> plants and the safety of clinical medication. Furthermore, this method may provide the UPLC-MS/MS evidence for the differentiation of the main close relative varieties of genus <i>Ajuga</i> according to these plants contain different mixtures of the four marker compounds.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":null,"pages":null},"PeriodicalIF":3.4,"publicationDate":"2024-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140058917","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"BSA nanoclusters-based sensor for detection of dopamine in schizophrenia from biofluids.","authors":"Bhakti Khanolkar, Pravin Shende","doi":"10.1080/03639045.2024.2328722","DOIUrl":"10.1080/03639045.2024.2328722","url":null,"abstract":"<p><strong>Objective: </strong>To develop nontoxic and stable fluorescent emission B-Cu nanoclusters (NCs) for the specific detection of dopamine at low concentrations in cerebrospinal fluid (CSF).</p><p><strong>Significance: </strong>Fluorescent gold and copper NCs conjugated with proteins, such as bovine serum albumin (BSA), offer photostability and healthcare potential. This study focused on fabricating B-Cu NCs that exhibited superior characteristics for sensitive dopamine detection.</p><p><strong>Methods: </strong>The study employed various instrumental techniques including attenuated total reflectance Fourier-transform infrared spectroscopy (ATR-FTIR), scanning electron microscopy (SEM), spectrofluorometry, and transmission electron microscopy (TEM) to characterize the formulated B-Cu NCs. The NCs were synthesized, resulting in particle size ∼300 nm. The highest observed fluorescence was recorded at 24542.81 relative fluorescence units (RFU).</p><p><strong>Results: </strong>The introduction of dopamine at concentrations of 0.1, 0.2, 0.3, and 0.4 ng/mL led to decreased fluorescence in both B-Au and B-Cu NCs due to an electron transport system. This reduction in fluorescence allowed dopamine concentration analysis in phosphate buffer and biological fluids such as blood plasma and CSF. B-Cu NCs showed potential as a biosensing system for point-of-care (POC) applications, specifically for diagnosing schizophrenia.</p><p><strong>Conclusion: </strong>The study successfully synthesized stable and nontoxic B-Cu NCs with enhanced fluorescent emission properties. These NCs exhibited the capacity to detect dopamine at low concentrations in CSF. The study's findings hold promise for future applications, particularly in the development of a B-Cu NCs-based biosensing system for convenient POC detection of schizophrenia by both patients and clinicians. The potential impact of this technology on healthcare and biomedical fields is substantial.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":null,"pages":null},"PeriodicalIF":3.4,"publicationDate":"2024-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140101256","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Formulation and optimisation of Ozenoxacin topical nano-emulgel including a comprehensive methodology to qualify and validate the critical parameters of an <i>in-vitro</i> release test method and <i>ex-vivo</i> permeation test.","authors":"Amarnath Reddy Ramireddy, Dilip Kumar Behara","doi":"10.1080/03639045.2024.2327466","DOIUrl":"10.1080/03639045.2024.2327466","url":null,"abstract":"<p><strong>Objective: </strong>The purpose of this study was to formulate, optimize Ozenoxacin topical nano-emulsion using factorial design followed by to prepare and evaluate nano-emulgel using validated <i>in-vitro</i> release testing (IVRT) technique for determination of Ozenoxacin release rate along with <i>ex-vivo</i> permeation testing (EVPT).Significance: Nano-emulgel is a proven delivery system for poorly soluble substances works by enhancing the solubility and bioavailability. Factorial design provides a systematic and efficient means to study the effect of multiple factors on responses. IVRT is an USP compendia technique utilized for performance analysis of semi-solid formulations.</p><p><strong>Methods: </strong>Nano-emulsion formulation optimization was done with factorial design, evaluated for globule size and % entrapment efficiency (EE). Nano-emulgels were characterized for assay, organic impurities, rheological behavior, IVRT, EVPT, and skin retention studies. IVRT validation was executed using vertical diffusion cells (VDCs).</p><p><strong>Results: </strong>Ozenoxacin nano-emulsion was optimized with 1:1 ratio of Oil: S_mix, 3:1 ratio of Surfactant:Co-Surfactant, and 15000 RPM of homogenization speed which resulted 414.6 ± 5.2 nm globule size and 92.8 ± 2.1% entrapment efficiency. Results confirmed that IVRT and Reversed Phase - High Performance Liquid Chromatographic techniques were validated as per regulatory guidelines. <i>In-vitro</i>, <i>ex-vivo</i> drug release, and skin retention from the optimized nano-emulgel formulation was comparatively higher (∼1.5 times) than that from the innovator (OZANEX^TM) formulation.</p><p><strong>Conclusions: </strong>Based on these results, Ozenoxacin nano-emulgel can be considered an effective alternative and was found to be stable at 40 °C/75% RH and 30 °C/75% RH storage condition for 6 months.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":null,"pages":null},"PeriodicalIF":3.4,"publicationDate":"2024-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140065050","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Exposure to potentially harmful excipients in medications among neonates at a state hospital in Malaysia.","authors":"Shien Woan Wong, Soo Piing Chew, Siti Azdiah Abdul Aziz, Noraida Mohamed Shah","doi":"10.1080/03639045.2024.2327462","DOIUrl":"10.1080/03639045.2024.2327462","url":null,"abstract":"<p><strong>Objectives: </strong>This study aimed to determine the incidence, types and predictors of Potentially Harmful Excipients (PHE) exposure among hospitalized neonates.</p><p><strong>Methods: </strong>A prospective observational study was conducted from March to April 2022 in neonatal wards at a state hospital in Malaysia. The PHEs of interest were aspartame, benzalkonium chloride, benzyl alcohol, benzoic acid or benzoates, ethanol, parabens, polysorbate 80, propylene glycol, saccharin sodium, sorbitol and sulfites. Product information leaflets (PILs) and summaries of product characteristics (SPCs) were referred to obtain information on active pharmaceutical ingredient, strength, trade name as well as type and amount of the excipients.</p><p><strong>Results: </strong>A total of 108 neonates were recruited and 97.2% of them were exposed to at least one PHE. Parabens (47.2%) and sulfites (27.5%) were the two most commonly administered PHEs. Benzyl alcohol is contraindicated in neonates but was administered to 8% of neonates in this study. The median daily dose of ethanol (24.11 mg/kg/day, IQR 19.73, 28.49) exceeded the acceptable daily intake (ADI) by four times. However, the dose was not available for all PHEs as this information is not always available in the PIL or SPC. Administration of cardiovascular drugs was associated with a higher risk of exposure to any PHE (OR 6.38, CI 2.75, 14.79, p-value < 0.001).</p><p><strong>Conclusion: </strong>The exposure of PHE among neonates in this study is high with certain PHEs exceeding the ADI. It highlights the need for certain strategies to be implemented to reduce such exposure in neonates.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":null,"pages":null},"PeriodicalIF":3.4,"publicationDate":"2024-03-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140065049","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Development, optimization and characterization of cisplatin loaded cubosomes for human lung carcinoma.","authors":"Hassaan Umar, Habibah A Wahab, Nadeem Ahmed, Nao Akusa Fujimura, Muhammad Wahab Amjad, Syed Nasir Abbas Bukhari, Waqas Ahmad","doi":"10.1080/03639045.2024.2326043","DOIUrl":"10.1080/03639045.2024.2326043","url":null,"abstract":"<p><strong>Objectives: </strong>This study aimed to develop, optimize and evaluate glyceryl monooleate (GMO) based cubosomes as a drug delivery system containing cisplatin for treatment of human lung carcinoma.</p><p><strong>Significance: </strong>The significance of this research was to successfully incorporate slightly water soluble and potent anticancer drug (cisplatin) into cubosomes, which provide slow and sustained release of drug for longer period of time.</p><p><strong>Methods: </strong>The delivery system was developed through top-down approach by melting GMO and poloxamer 407 (P407) at 70 °C and then drop-wise addition of warm deionized water (70 °C) containing cisplatin. The formulation then exposed to probe sonicator for about 2 min. A randomized regular two level full factorial design with help of Design Expert was used for optimization of blank cubosomal formulations. Cisplatin loaded cubosomes were then subjected to physico-chemical characterization.</p><p><strong>Results: </strong>The characterization of the formulation revealed that it had a sufficient surface charge of -9.56 ± 1.33 mV, 168.25 ± 5.73 nm particle size, and 60.64 ± 0.11% encapsulation efficiency. The <i>in vitro</i> release of cisplatin from the cubosomes at pH 7.4 was observed to be sustained, with 94.5% of the drug being released in 30 h. In contrast, 99% of cisplatin was released from the drug solution in just 1.5 h. <i>In vitro</i> cytotoxicity assay was conducted on the human lung carcinoma NCI-H226 cell line, the cytotoxicity of cisplatin-loaded cubosomes was relative to that of pure cisplatin solution, while blank (without cisplatin) cubosomes were nontoxic.</p><p><strong>Conclusions: </strong>The obtained results demonstrated the successful development of cubosomes for sustained delivery of cisplatin.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":null,"pages":null},"PeriodicalIF":3.4,"publicationDate":"2024-03-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140048999","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}