Drug Development and Industrial Pharmacy最新文献

{"title":"Comparison of oven drying and freeze drying methods for the production of fast melt films containing quetiapine fumarate.","authors":"Hiu Ching Phang, Zhi Qi Ng, Najwa Mohamad, Yik Ling Chew, Ashok Balaraman, Phei Er Kee, Kenji Mishima, Bey Hing Goh, Long Chiau Ming, Kai Bin Liew","doi":"10.1080/03639045.2024.2409168","DOIUrl":"10.1080/03639045.2024.2409168","url":null,"abstract":"<p><strong>Background: </strong>Quetiapine fumarate (QTP) is commonly prescribed for schizophrenic patient, typically available in tablet or oral suspension form, presenting challenges such as administration difficulties, fear of choking and distaste for its bitter taste. Fast melt films (FMF) offer an alternative dosage form with a simple development process, ease of administration and rapid drug absorption and action onset.</p><p><strong>Objective: </strong>This study aims to prepare FMF with different formulations using solvent casting methods and to compare the effects of different drying methods, including oven drying and freeze drying, on the properties of the films.</p><p><strong>Methods: </strong>Various formulations were created by manipulating polymer types (starch, hydroxypropyl methylcellulose (HPMC) and guar gum) at different concentrations, along with fixed concentrations of QTP and other excipients. Characterization tests including surface morphology, weight, thickness, pH, tensile strength, elongation length, Young's modulus, folding endurance and disintegration time were conducted. The optimal FMF formulation was identified and further evaluated for moisture and drug content, dissolution behavior, accelerated stability, X-ray diffraction (XRD), and palatability.</p><p><strong>Results: </strong>FMF containing 10 mg guar gum/film developed using oven drying emerged as the optimum choice, exhibiting desirable film appearance, ultra-thin thickness (0.453 ± 0.002 mm), appropriate pH for oral intake (pH 5.0), optimal moisture content of 11.810%, rapid disintegration (52.67 ± 1.53 s), high flexibility (folding endurance > 300 times) and lower Young's modulus (1.308 ± 0.214).</p><p><strong>Conclusion: </strong>Oven drying method has been proven to be favorable for developing FMF containing QTP, meeting all testing criteria and providing an alternative option for QTP prescription.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"810-826"},"PeriodicalIF":2.4,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142343507","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":"Olive oil and flaxseed oil incorporating niosomes for enhanced <i>in vivo</i> anti-diabetic efficacy of canagliflozin.","authors":"Ghada Saad, Gamal M El Maghraby, Amal A Sultan","doi":"10.1080/03639045.2024.2409167","DOIUrl":"10.1080/03639045.2024.2409167","url":null,"abstract":"<p><strong>Background: </strong>Canagliflozin (CFZ) is broadly implicated for the management of type 2 diabetes mellitus. Unfortunately, it has low oral bioavailability due to poor solubility behavior and restricted membrane permeability.</p><p><strong>Objective: </strong>The current work focuses on development of CFZ encapsulated niosomes for enhanced oral anti-diabetic efficacy.</p><p><strong>Methodology: </strong>Niosomes comprising Span 60 and cholesterol were formulated both in absence and presence of olive oil or flaxseed oil. These were evaluated <i>in vitro</i> for average vesicular size, structural morphology, CFZ entrapment efficiency, and drug release. Additionally, the oral hypoglycemic effect of CFZ encapsulated niosomes was explored in diabetic rats.</p><p><strong>Results: </strong>The fabricated niosomes were negatively charged spherical vesicles with a size range of 103.0-141.7 nm. These entrapped CFZ with efficiency ranging from 92.3% to 96.0%. Drug release investigations reflected that incorporating CFZ into niosomes significantly sustained drug release compared to the aqueous drug dispersion. Oral administration of niosomal formulations significantly enhanced the oral antidiabetic effect of CFZ. Comparing the tested niosomes, similar efficiency was shown eliminating the effect of composition.</p><p><strong>Conclusion: </strong>The enhanced oral bioavailability of niosomes' encapsulated drugs is related to niosomal vesicular structure which allows intact niosomes absorption. The study presented niosomes as promising carriers for improved oral anti-diabetic activity of CFZ.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"801-809"},"PeriodicalIF":2.4,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142343508","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":"Fabrication and optimization of naringin-loaded MOF-5 encapsulated by liponiosomes as smart drug delivery, cytotoxicity, and apoptotic on breast cancer cells.","authors":"Lina M Alneghery, Mohammed Al-Zharani, Fahd A Nasr, Zienab E Eldin, Tayel A Al Hujran, Hesham M Tawfeek, Mohamed H Fayed, Shehab Elbeltagi","doi":"10.1080/03639045.2024.2388786","DOIUrl":"10.1080/03639045.2024.2388786","url":null,"abstract":"<p><strong>Introduction: </strong>Cancers are regarded as hazardous due to their high worldwide death rate, with breast cancer (BC), which affects practically all cancer patients globally, playing a significant role in this statistic. The therapeutic approach for BC has not advanced using standard techniques, such as specialized naringin (NG) chemotherapy. Instead, a novel strategy has been utilized to enhance smart drug delivery (SDD) to tumors.</p><p><strong>Significance: </strong>Herein, we established NG-loaded zinc metal-organic framework-5 (NG-MOF-5) coated with liponiosomes (LNs) to manufacture NG-MOF-5@LNs nanoparticles (NPs) for antibacterial and cancer treatment.</p><p><strong>Methods: </strong>MOF-5, NG, and NG-MOF-5@LNs were evaluated with XRD, thermogravimetric analysis (TGA), FTIR, SEM, TEM, PDI, ZP, encapsulation efficiency (EE), loading efficiency (LE), and drug release (DR) kinetics. We examined the antibacterial activity involving minimum inhibitory concentration (MIC) and zone of inhibition by NG, MOF-5, and NG-MOF-5@LNs. The cell viability, necrosis, and total apoptosis (late and early) were evaluated for anti-cancer activity against MCF-7 BC cells.</p><p><strong>Results: </strong>TEM results demonstrated that NG-MOF-5@LNs formed monodispersed spherical-like particles with a size of 122.5 nm, PDI of 0.139, and ZP of +21 mV. The anti-microbial activity results indicated that NG-MOF-5@LNs exhibited potent antibacterial effects, as evidenced by inhibition zones and MIC values. The Higuchi model indicates an excellent fit (<i>R</i>² = 0.9988). The MTT assay revealed anti-tumor activity against MCF-7 BC cells, with IC₅₀ of 21 µg/mL for NG-MOF-5@LNs and demonstrating a total apoptosis effect of 68.2% on MCF-7 cells.</p><p><strong>Conclusion: </strong>NG-MOF-5@LNs is anticipated to show as an effective antimicrobial and novel long-term-release antitumor agent and might be more suitable for MCF-7 cell therapy.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-14"},"PeriodicalIF":2.4,"publicationDate":"2024-08-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141888763","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":"Stability-indicating green HPLC method for fixed-dose tablets containing remogliflozin etabonate and teneligliptin: an AQbD approach.","authors":"Raj Patel, Rajendra Kotadiya","doi":"10.1080/03639045.2024.2400199","DOIUrl":"10.1080/03639045.2024.2400199","url":null,"abstract":"<p><strong>Background: </strong>In June 2021, the Central Drug Standards Control Organization approved a fixed-dose combination tablet containing remogliflozin etabonate (100 mg) and teneligliptin (10 mg) to manage type II diabetes.</p><p><strong>Objective: </strong>This study aims to develop a stability-indicating RP-HPLC method for quantifying remogliflozin etabonate and teneligliptin in tablet formulations <i>via</i> analytical quality by design (AQbD) principles.</p><p><strong>Methods: </strong>Risk assessment, Plackett-Burman design, and central composite design were employed to understand the impact of independent variables on critical analytical attributes. The stationary phase was a HyperClone BDS C18 column, and the mobile phase consisted of acetonitrile and phosphate buffer (20 mM, pH 5) at a 45:55% (v/v) ratio.</p><p><strong>Results: </strong>The method, validated per ICH Q2 (R1), resulted in retention times of 3.395 and 12.308 min for teneligliptin and remogliflozin etabonate, respectively. Forced degradation studies confirmed robustness, with clear peak separation and no interference from degradation products. The AGREE score of 0.65 supports its green applicability for tablet analysis in quality control.</p><p><strong>Conclusion: </strong>The AQbD-assisted RP-HPLC method developed in this study offers environmental friendliness, efficient separation with well-defined peaks, and simple mobile phase combination.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"750-762"},"PeriodicalIF":2.4,"publicationDate":"2024-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142125131","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":"Nanocrystal formulations of mebendazole employing quality by design and molecular level insights by atomistic simulations.","authors":"Elisavet Vardaka, Kyriakos Kachrimanis","doi":"10.1080/03639045.2024.2398597","DOIUrl":"10.1080/03639045.2024.2398597","url":null,"abstract":"<p><strong>Objective: </strong>The present study investigates the production of mebendazole nanocrystal formulations by wet media milling.</p><p><strong>Significance: </strong>Nanocrystal formulations are expected to enhance the dissolution properties of mebendazole, which possesses poor solubility, highly dependent on crystal polymorphism.</p><p><strong>Methods: </strong>A Box-Behnken design was employed to study the effects of formulation and process variables on the nanocrystal size and ζ-potential. The optimal nanosuspensions were solidified by spay-drying and freeze-drying with and without mannitol, and the effects of the drying method on the reconstitution of the nanosuspension was studied. Additionally, their physicochemical properties were determined, while the mechanism of fracture and stabilizer adsorption were investigated by atomistic simulations.</p><p><strong>Results: </strong>Poloxamer 407 is the most suitable stabilizer, while the bead size, milling speed, and stabilizer content significantly affect the diameter. The ζ-potential is affected by the stabilizer concentration depending on bead size. Energy-vector diagrams revealed a slip plane in the lattice of form C, while molecular dynamics simulations revealed strong interactions between stabilizer and crystal surface. Both drying processes induce polymorphic transformation to form A, which, however, can be partially prevented by the addition of mannitol in freeze-drying, at the expense of suspension redispersibility. The spray-dried nanosuspensions exhibited substantially enhanced dissolution profile compared to neat mebendazole, probably due to reduction of particle size, despite transformation to the unfavorable form A.</p><p><strong>Conclusions: </strong>Nanocrystal formulations exhibited significant dissolution enhancement, while experimental design and atomistic simulations provided useful insights into the mechanism of their formation and stability.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"735-749"},"PeriodicalIF":2.4,"publicationDate":"2024-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142105394","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":"Industrial manufacturing method and characterization of Ayurvedic marine drugs: mother pearl, cowry, coral and pearl.","authors":"Sandeep Chavan, Sushama Bhuvad, Vidya Gupta, Vineeta Deshmukh, Sadanand Sardeshmukh","doi":"10.1080/03639045.2024.2396902","DOIUrl":"10.1080/03639045.2024.2396902","url":null,"abstract":"<p><strong>Introduction: </strong>Ayurvedic marine drugs derived from mollusc shells and coral are regularly used by Ayurvedic physicians to treat several disease conditions like acid peptic disease, irritable bowel syndrome, osteoporosis, etc. However, standard operating procedures for manufacturing these drugs and their complete characterization have not been published in the Ayurvedic Formulary and Ayurvedic Pharmacopeia of India to date.</p><p><strong>Methods: </strong>Present study describes the traditional manufacturing process and thorough characterization using classical and advanced analytical tools. The raw materials characters, in-process parameters, and finished product specifications have been elaborated to develop monographs. Especially, the identity and purity of raw coral and pearl were checked by Raman Spectroscopy and Energy Dispersive X-ray Fluorescence analysis.</p><p><strong>Results: </strong>In the finished product analysis, the X-Ray Diffraction study revealed that incineration after trituration with <i>Aloe barbadensis</i> leaf pulp or rose water converted the aragonite phase of calcium carbonate into calcite phase in mother pearl, cowry, and pearl while the calcite form of raw coral was retained. The prominent bands around 1390, 870, and 712 cm^-1 detected by Fourier Transform-Infrared Spectroscopy and mass loss between 39-44% (w/w) revealed by thermogravimetric analysis confirmed the carbonate form of these calcium-based drugs. The finished products were very fine grayish-white powders constituted by irregularly shaped nano-micro particulate calcium carbonate exhibiting particle size between 600 nm (D10 value) to 1.2 µm (D90 value).</p><p><strong>Conclusion: </strong>The quality control and assurance achieved in this study may be further utilized by the pharmaceutical industries to manufacture quality marine drugs and conduct efficacy studies.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"721-734"},"PeriodicalIF":2.4,"publicationDate":"2024-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142105393","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":"Correction.","authors":"","doi":"10.1080/03639045.2024.2406315","DOIUrl":"10.1080/03639045.2024.2406315","url":null,"abstract":"","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"i"},"PeriodicalIF":2.4,"publicationDate":"2024-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142281918","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":"Correction.","authors":"","doi":"10.1080/03639045.2024.2416335","DOIUrl":"10.1080/03639045.2024.2416335","url":null,"abstract":"","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"776"},"PeriodicalIF":2.4,"publicationDate":"2024-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142496930","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":"Modeling moisture change of packaged dry tablet dosage forms under consumer use condition.","authors":"Duck Soon An, Dong Sun Lee","doi":"10.1080/03639045.2024.2382415","DOIUrl":"10.1080/03639045.2024.2382415","url":null,"abstract":"<p><p>A simple mathematical model based on product's moisture sorption isotherm and package's moisture transmission was developed to predict moisture content of dry solid tablets during consumers' use, which is useful for determination of in-use shelf life (ISL) or secondary shelf life. The moisture increase depending on amount of product remaining in the package was accounted for in the mass balance equation on the package. The model was first verified by literature data of desiccant canisters in a plastic bottle of high density polyethylene exposed to two environmental conditions (25 °C and 60% relative humidity (RH); 40 °C and 75% RH) simulating in-use of removing one canister each day. Then an experimental work was conducted on dry refresher candies in a polyethylene terephthalate bottle at 25 °C with two tablets taken out every day, which confirmed the model's capability to predict the product moisture content during in-use storage of 76% and 90% RH. Its use can provide science-based accurate determination of ISL, which may work as consumer guideline. The model is also expected to be helpful for recommending management scheme of whole product life.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"639-645"},"PeriodicalIF":2.4,"publicationDate":"2024-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141726963","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":"Phytochemical profiling and antioxidant evaluation of <i>Rhododendron arboreum</i> Sm leaf and flower: integrative analysis using advanced analytical techniques.","authors":"Yangchen Dolma Kom, Karthiyayini Ramaswamy, Surya Suresh","doi":"10.1080/03639045.2024.2390029","DOIUrl":"10.1080/03639045.2024.2390029","url":null,"abstract":"<p><strong>Objective: </strong>This study investigates the biological activities of <i>Rhododendron arboreum</i> Sm from the eastern Himalayas, addressing a literature gap on its properties. It explores the plant's phytochemical, antioxidant, and medicinal characteristics.</p><p><strong>Significance: </strong>Evaluating methanolic extracts of <i>R. arboreum</i> offers valuable insights into its bioactive potential. Comprehensive GC-MS analysis identified a diverse array of compounds, highlighting the plant's chemical composition.</p><p><strong>Methods: </strong>Methanolic leaf and flower extracts underwent sequential extraction and phytochemical profiling using column chromatography, TLC, and GC-MS analysis. Spectral studies aided compound identification, and antioxidant activity was assessed <i>via</i> spectrophotometric assays.</p><p><strong>Results: </strong>Column chromatography separated methanol leaf and flower extracts into 17 and 24 distinct fractions, respectively. TLC analysis showed specific R_f values for leaf (0.58, 0.65, 0.75, 0.8, 0.86, 0.9) and flower samples (0.91, 0.38, 0.48, 0.51, 0.56, 0.6, 0.65, 0.75, 0.85, 0.96). GC-MS analysis revealed a variety of organic functional groups, including aliphatic hydrocarbons, aromatic compounds, heterocyclic molecules, phenolic compounds, steroids, terpenoids, alcohols, esters, and other bioactive compounds. FTIR spectra identified functional groups such as hydroxyls, primary amines, alkanes, and alkynes. NMR data indicated a complex molecular composition with diverse proton environments. Leaf extracts demonstrated superior antioxidant activity compared to flower extracts in DPPH, ABTS, hydrogen peroxide scavenging, lipid peroxidation inhibition, and FRAP assays.</p><p><strong>Conclusion: </strong>The study identifies diverse phytochemicals in <i>R.arboreum</i> extracts and highlights their potential applications in pharmaceuticals, nutraceuticals, and functional foods, owing to the superior antioxidant activity of leaf extracts compared to flowers.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"687-705"},"PeriodicalIF":2.4,"publicationDate":"2024-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141901280","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}