RSC Pharmaceutics最新文献

{"title":"Lysozyme activated co-delivery of latanoprost–timolol from mucoadhesive chitosan nanocomposite to manage glaucoma†","authors":"B. N. Kumara, R. Shambhu, Yoon-Bo Shim and K. Sudhakara Prasad","doi":"10.1039/D4PM00031E","DOIUrl":"https://doi.org/10.1039/D4PM00031E","url":null,"abstract":"<p >Glaucoma is a leading cause of irreversible blindness, and controlling intraocular pressure is imperative for good clinical outcomes. It is important to use natural stimuli to trigger the release of the drug when it is linked to a nanoparticle/nanocomposite, particularly in ophthalmic applications to maintain sustained release. Herein the preparation and investigation of biocompatible, mucoadhesive dual drug-loaded chitosan (CS)–graphene quantum dot (GQD) nanocomposites are reported. Drug release from the nanocomposite was controlled by the presence of a natural lacrimal fluid enzyme, lysozyme (Lyz). Lyz is efficient at cleaving the β-1,4 glycosidic linkages of CS, thereby releasing the drug of interest. A biocompatible, fluorescent nanomaterial <em>i.e.</em>, GQDs, was employed to track drug loading by using simple photoluminescent spectral studies. The optimized nanocomposite encapsulation efficiencies (EEs) were 94.51% and 74.08% for latanoprost (LP) and timolol (TM) and delivered 32.68% and 66.61% of drugs, respectively, in 72 h. Dual drug delivery through the cleavage of β-1,4 glycosidic linkages of CS in the presence of Lyz was confirmed through <small>¹</small>H-NMR and FE-SEM studies. An increase in the particle size from 490 nm to 1584 nm in the presence of mucin supports the mucoadhesiveness of the nanocomposite. The <em>in vitro</em> cytocompatibility and live/dead staining assays against human corneal epithelial (HCE) cells showed ≥80% cell viability. <em>Ex vivo</em> tests proved that the nanocomposite was non-irritant, and histopathological studies showed normal growth of blood vessels. Molecular docking studies showed the hydrogen bonding and electrostatic interactions between the drug and CS. Hence the developed nanocomposite could be used as an ocular suspension or nanocomposite for further preclinical studies on glaucoma management.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 3","pages":" 548-569"},"PeriodicalIF":0.0,"publicationDate":"2024-05-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/pm/d4pm00031e?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141980177","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":"Acid- and base-resistant antimicrobial hydrogels based on polyoxometalates and chitosan†","authors":"Callum McWilliams, Isabel Franco-Castillo, Andrés Seral Ascaso, Sonia García-Embid, Mariella Malefioudaki, Johann G. Meier, Rafael Martín-Rapún and Scott G. Mitchell","doi":"10.1039/D4PM00062E","DOIUrl":"https://doi.org/10.1039/D4PM00062E","url":null,"abstract":"<p >Invasive fungal infections kill more than 1.7 million and affect over a billion people each year; however, their devastating impact on human health is not widely appreciated and frequently neglected by public health authorities. In 2022, the WHO highlighted the urgent need for efficient diagnostic tests as well as safe and effective new compounds, drugs, and vaccines. Our hypothesis was that the naturally occurring polymer chitosan (CS) could be combined with molecular polyoxometalates (POMs) to produce POM@CS hybrid materials to promote broad-spectrum activity and habilitate synergic effects, which will ultimately help to prevent the appearance of resistances. Here we report the synthesis, characterisation, and antimicrobial activity of POM@CS hydrogels. Spectroscopic (FT-IR &amp; EDS) and electron microscopy (SEM &amp; TEM) techniques revealed the structural composition and morphology of the hybrid materials, whilst dynamic mechanical analysis demonstrated that the mechanical properties of the hydrogels were stable between pH 2 and 10 and were highly resistant to acidic conditions. The POM@CS hydrogels were active against Gram-positive <em>Bacillus subtilis</em> and Gram-negative <em>Escherichia coli</em> bacteria, and proved to completely reduce fungal growth of <em>Aspergillus niger</em> and <em>Cladosporium cladosporioides</em>. Furthermore, the antimicrobial activity of the hydrogels could be enhanced through the inclusion of naturally occurring antimicrobial agents such as eugenol and cinnamaldehyde. Altogether, the development of such surface-active antimicrobial hydrogels pave the way to functional materials that can prevent biofilm formation in health and environmental applications and contribute to reducing the spread of antimicrobial resistance.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 4","pages":" 755-764"},"PeriodicalIF":0.0,"publicationDate":"2024-05-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/pm/d4pm00062e?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142434701","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":"Doxorubicin-Polysorbate 80 conjugates: targeting effective and sustained delivery to the brain†","authors":"S. Ram Prasad, Sruthi Sudheendran Leena, Ani Deepthi, A. N. Resmi, Ramapurath S. Jayasree, K. S. Sandhya and A. Jayakrishnan","doi":"10.1039/D4PM00053F","DOIUrl":"https://doi.org/10.1039/D4PM00053F","url":null,"abstract":"<p >Targeting therapeutic agents to the brain to treat central nervous system (CNS) diseases is a major challenge due to the blood–brain barrier (BBB). In this study, an attempt was made to deliver a model drug such as doxorubicin (DOX), to the brain in a mouse model through DOX-Polysorbate 80 (DOX-PS80) conjugates. DOX was successfully conjugated with the non-ionic surfactant Polysorbate 80 (PS80) by carbamate linkage and the conjugate was characterized by different spectroscopic techniques, such as FTIR, UV-Visible and NMR. The DOX conjugation efficacy was found to be 43.69 ± 4.72%. The <em>in vitro</em> cumulative release of DOX from the conjugates was found to be 4.9 ± 0.8% in PBS of pH 7.3 and 3.9 ± 0.6% in simulated cerebrospinal fluid (CSF) of pH 7.3 at the end of 10 days. An <em>in vitro</em> BBB permeability assay was carried out using bEnd.3 cells and DOX-PS80 conjugate showed a 3-fold increase in BBB permeability compared with controls. <em>In vitro</em> cytotoxicity assay using U251 human glioblastoma cells showed an IC<small>₅₀</small> value of 38.10 μg mL<small>⁻¹</small> for DOX-PS80. Cell uptake studies revealed that DOX-PS80 was effectively taken up (90%) by the bEnd.3 and U251 cells and localized in cytoplasm at the end of 24 h. Pharmacokinetic parameters for DOX-PS80 were evaluated using <em>in silico</em> studies. Tumor spheroid assay and <em>in vivo</em> experiments in Swiss albino mouse demonstrated the possibility of DOX-PS80 conjugate crossing the BBB and delivering the drug molecules to the target site for treating CNS disorders.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 3","pages":" 412-429"},"PeriodicalIF":0.0,"publicationDate":"2024-05-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/pm/d4pm00053f?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141980149","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":"Novel pH-sensitive gum ghatti-cl-poly(acrylic acid) composite hydrogel based on graphene oxide for metformin hydrochloride and sodium diclofenac combined drug-delivery systems†","authors":"Pragnesh N. Dave and Pradip M. Macwan","doi":"10.1039/D3PM00072A","DOIUrl":"https://doi.org/10.1039/D3PM00072A","url":null,"abstract":"<p >The objective of the present study was to synthesize pH-sensitive gum ghatti-<em>cl</em>-poly (acrylic acid)/GO hydrogels for the drug delivery and controlled combined release of metformin hydrochloride and sodium diclofenac. Gum ghatti (Gg) and acrylic acid (AA) were free radicals copolymerized using <em>N,N</em>‘-methylenebisacrylamide (MBA) and tetramethyl ethylenediamine as cross-linkers and ammonium persulfate (APS) as an initiator. The structure and surface morphology of the composite hydrogel were determined using FTIR and SEM analyses, respectively. The FTIR studies confirmed the successful acrylic acid and graphene oxide grafting and drug binding onto the backbone of the synthesized hydrogel. Drug-release kinetics and mechanisms were investigated using zero- and first-order kinetic models as well as the Korsmeyer–Peppas model, Higuchi model, and Hixson–Crowell model. Drug-release experiments revealed the important characteristics related with physiologically expected pH levels, including a high release rate at pH 9.2. At pH 9.2, metformin HCl drug release increased from 4.68% to 37.46%, whereas sodium diclofenac release increased from 3.25% to 54.75%. However, at pH 9.2, both metformin hydrochloride and sodium diclofenac showed non-Fickian transport mechanisms. In summary, combining drugs may reduce the efficacy of a single medication while influencing metabolic rescue mechanisms.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 2","pages":" 357-371"},"PeriodicalIF":0.0,"publicationDate":"2024-05-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/pm/d3pm00072a?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141424753","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":"Potential of ultrasonic processing in biomedical applications","authors":"Siddhi Lokhande, Bhagyashree V. Salvi and Pravin Shende","doi":"10.1039/D4PM00010B","DOIUrl":"https://doi.org/10.1039/D4PM00010B","url":null,"abstract":"<p >Ultrasound waves are sound waves with frequencies higher than the human audible frequencies and application of these waves in biomedical science is explored in this article. A novel approach that involved the use of ultrasound was discovered in around 1950 and since then, it is experimented on to obtain various applications like gene/drug delivery, diagnosis, theranostics, tissue engineering, <em>etc</em>. Ultrasound waves are sound waves travelling at frequencies above human audible frequencies and are further classified into three types: high frequency, medium frequency and low frequency, each showing different therapeutic applications. Ultrasound has shown its application in various fields like dentistry, wastewater management, <em>etc</em>. Apart from therapeutic use, ultrasound is also implemented in synthesis, extraction, tissue engineering, gene delivery and many more applications. This article mentions the recent applications of ultrasound as a non-invasive route for the treatment of several diseases also due to its enhanced penetration of cells which helped greatly in the delivery of drugs/genes, in the extraction of various essential biological components from plants, in the synthesis of several compounds, in the field of theranostics – a combination of diagnosis and therapy, in tissue engineering, <em>etc</em>.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 2","pages":" 204-217"},"PeriodicalIF":0.0,"publicationDate":"2024-05-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/pm/d4pm00010b?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141424766","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":"Fabrication of miconazole nitrate solid lipid nanoparticle loaded microneedle patches for the treatment of Candida albicans biofilms","authors":"Muhammad Sohail Arshad, Aqsa Ayub, Saman Zafar, Sadia Jafar Rana, Syed Aun Muhammad, Ambreen Aleem, Ekhoerose Onaiwu, Kazem Nazari, Ming-Wei Chang and Zeeshan Ahmad","doi":"10.1039/D4PM00042K","DOIUrl":"https://doi.org/10.1039/D4PM00042K","url":null,"abstract":"<p >The present study aimed to develop miconazole nitrate solid lipid nanoparticle (SLN) loaded polymeric microneedle (MN) patches (SPs) <em>via</em> the vacuum micromolding approach. The SLNs were fabricated through melt emulsification of stearic acid using Tween 80. SPs were prepared using chitosan, gelatin (as base materials) and polyethylene glycol 400 (as a plasticizer). The prepared formulations were evaluated for various physicochemical parameters, including particle size, polydispersity index, encapsulation efficiency, loading capacity (in the case of SLNs), folding endurance, % swelling and insertion ability (in the case of SPs). Scanning electron microscopy and differential scanning calorimetry (DSC) studies were carried out for morphological and thermal analysis, respectively. Phase analysis was carried out <em>via</em> X-ray diffraction (XRD). <em>In vitro</em> tensile strength, drug release, anti-biofilm activity and <em>in vivo</em> anti-biofilm activity were studied to assess the efficiency of the SLN loaded polymeric formulation. Miconazole nitrate containing SLNs appeared as smooth-surfaced aggregates and displayed a particle diameter of ∼224 nm, polydispersity index of ∼0.32, encapsulation efficiency of ∼88.88% and loading capacity of ∼8.88%. SPs exhibited evenly aligned, uniform-surfaced, sharp-tipped projections, with an acceptable folding endurance of ∼300 and % swelling of ∼359%. DSC and XRD results confirmed the incorporation of the drug within the solidified lipid matrix as an amorphous solid. The miconazole nitrate lipidic nanoparticle containing polymeric formulation exhibited a tensile strength ∼1.35 times lower than the pure drug loaded counterpart. During <em>in vitro</em> studies, SPs released ∼94% miconazole nitrate within 150 minutes and reduced the mass of the <em>Candida albicans</em> (<em>C. albicans</em>) biofilm by ∼79%. After 10 days of treatment with SPs, <em>C. albicans</em> infected wounds were healed, confirming that the prepared formulations can be used for the management of fungal biofilms.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 3","pages":" 458-471"},"PeriodicalIF":0.0,"publicationDate":"2024-05-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/pm/d4pm00042k?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141980157","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":"Evaluation of the anti-depressant potential of EGCG-loaded nanoparticles in unstressed and stressed mice","authors":"Shakti Dahiya, Ruma Rani, Neeraj Dilbaghi, Dinesh Dhingra, Sant Lal and Jaya Verma","doi":"10.1039/D3PM00022B","DOIUrl":"https://doi.org/10.1039/D3PM00022B","url":null,"abstract":"<p >Epigallocatechin-3-gallate (EGCG) is a key bio-active component of green tea and has demonstrated significant antidepressant activity in laboratory animals. Nano-particulate drug delivery offers great potential to overcome drawbacks associated with EGCG <em>i.e.</em> its low solubility and stability by transforming it into effective deliverable drugs. In the current study, nano-formulations of EGCG alone and with piperine were synthesized using antisolvent precipitation methodology followed by evaluation of their <em>in vivo</em> antidepressant effect in unstressed and stressed Swiss male albino mice. The mice were exposed to distinct stressors <em>i.e.</em> tail pinch, induction of immobilization, <em>etc</em>. throughout a span of three weeks. Zein, a protein nanocarrier, was nano-encapsulated with EGCG (25 mg) and EGCG + piperine (25 mg + 5 mg). For a continuous three weeks, the mice were administered EGCG-loaded nanosuspensions (25 mg kg<small>⁻¹</small>) and EGCG–piperine nanocomplexes (25 mg kg<small>⁻¹</small>). To determine the impact of various medication treatments on stressed and unstressed mice, the tail suspension test (TST) was employed as a behavioural paradigm. Mice exposed to various drug treatments were also evaluated for the effect on locomotor activity. The animals were euthanized followed by further estimation of plasma corticosterone, plasma nitrite, brain malondialdehyde, brain MAO-A, brain reduced glutathione, and brain catalase levels. The EGCG–piperine nanocomplex (25 mg kg<small>⁻¹</small>) and paroxetine HCl (10 mg kg<small>⁻¹</small>) <em>per se</em> significantly reduced immobility time in unstressed and stressed mice as compared to their respective control groups treated with a vehicle. However, in the case of locomotor activity, no significant effect was observed. EGCG loaded nanosuspension, EGCG–piperine nanocomplex and paroxetine HCl significantly decreased plasma nitrite, and brain MAO-A, brain malondialdehyde and brain catalase levels. However, these drug treatments significantly increased plasma corticosterone and brain reduced glutathione levels in unstressed and stressed mice as compared to their respective control groups treated with a vehicle. So, the intraperitoneal administration of nanoformulations synthesized using EGCG alone and along with piperine significantly improves the antidepressant-like behavior in mice.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 2","pages":" 344-356"},"PeriodicalIF":0.0,"publicationDate":"2024-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/pm/d3pm00022b?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141424761","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 a naproxen and gaultheria oil based topical nanoemulsion for the amelioration of osteoarthritis†","authors":"Abdul Nafey Faheem, Ahsan Ali, Athar Shamim, Sradhanjali Mohapatra, Ayesha Siddiqui, Zeenat Iqbal and Mohd. Aamir Mirza","doi":"10.1039/D4PM00059E","DOIUrl":"https://doi.org/10.1039/D4PM00059E","url":null,"abstract":"<p >Osteoarthritis (OA) is a chronic degenerative condition characterized by the wearing down of the articulating surfaces of the tibia–femoral joint. It involves the breakdown of cartilage, leading to a reduction in joint space, primarily affecting the medial aspect of the joint. Treatment options for OA include oral and topical medications, as well as chemical and surgical interventions. Among potential treatments, naproxen (NAP) and gaultheria oil (GO) have shown promising anti-inflammatory effects. However, NAP's distribution is hindered by its limited solubility and poor penetration. Additionally, there is no marketed product or published report of any combination product of GO with any synthetic drug. Hence a novel nanoemulsion (NE) based gel has been developed. For NE development, Tween 80 and PEG 400 were selected as the surfactant and co-surfactant, respectively. The particle size, polydispersity index (PDI) and zeta potential were found to be 209.2 nm, 0.2119, and −24.7 mV respectively. <em>In vitro</em> cumulative drug release in the initial 24 h was 95.64 ± 0.75% for NE and 87.44 ± 0.84% for NEG. Similarly, <em>in vitro</em> drug permeation after 24 h was 17.447 μg cm<small>⁻²</small> and 9.3287 μg cm<small>⁻²</small>, respectively. The rheological behavior, skin irritation, and stability of the NEG were also evaluated.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 3","pages":" 498-512"},"PeriodicalIF":0.0,"publicationDate":"2024-04-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/pm/d4pm00059e?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141980160","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":"In vitro evaluation of microneedle strength: a comparison of test configurations and experimental insights","authors":"Bilal Harieth Alrimawi, Jing Yi Lee, Keng Wooi Ng and Choon Fu Goh","doi":"10.1039/D4PM00024B","DOIUrl":"https://doi.org/10.1039/D4PM00024B","url":null,"abstract":"<p >To ensure the safe and effective application of microneedles for drug delivery to the skin, the mechanical properties the microneedles and their ability to penetrate the skin are critical quality control parameters. While <em>ex vivo</em> and <em>in vivo</em> evaluations may be valuable to demonstrate actual skin penetration, they can be costly and difficult to accomplish consistently due to the inherent biological variability of the skin. On the other hand, <em>in vitro</em> approaches provide a facile means of characterising the intrinsic mechanical properties of the microneedles, independent of such biological variability. Thus, they can be used to predict and screen for the <em>in vivo</em> and <em>ex vivo</em> performance of new microneedle formulations. A variety of experimental configurations has been reported in the literature focusing on mechanical evaluations including compression tests and <em>in vitro</em> microneedle insertion studies using a non-biological skin simulant, Parafilm® M. However, there has been a paucity of data that address the comparability of the various experimental configurations. Here, we evaluated several methods for assessing the mechanical properties of microneedles <em>in vitro</em>, including their ability to insert into a non-biological skin simulant under a defined axial force, and share some insights into the experimental design and data interpretation.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 2","pages":" 227-233"},"PeriodicalIF":0.0,"publicationDate":"2024-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/pm/d4pm00024b?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141424769","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":"Elucidation of processing parameters for the reverse engineering of tablets","authors":"Devendra Choudhary, Dnyaneshwar Kalyane, Suryanarayana Polaka, Tanisha Gupta and Rakesh Kumar Tekade","doi":"10.1039/D3PM00058C","DOIUrl":"https://doi.org/10.1039/D3PM00058C","url":null,"abstract":"<p >Reverse engineering can assist in decoding the formula and manufacturing parameters employed in innovator formulations. Generic pharmaceutical industries use it to develop generic cheaper versions of innovator tablets. Herein, we report the systematic application of reverse engineering in determining the manufacturing process utilized by innovators to prepare tablet formulations. The outcome inferred that the critical information such as the granulation and solvent type in the innovator formulation could be identified by systematic analysis <em>via</em> scanning electron microscopy (SEM) images and sieve and texture analysis. Furthermore, critical investigation of the levels of fines generated during sieve analysis could reveal the tablet manufacturing process. It was observed that the maximum amount of fines was generated in the case of post-compression granules obtained by tablets prepared by direct compression. The hardness of granules is yet another major factor that could help to delineate the type of drying technique used in innovator manufacturing. Granules obtained from crushing a tablet prepared by wet granulation with tray drying were harder than those prepared by drying on a fluidized bed dryer (FBD). The outcome of this investigation may be helpful for formulation scientists working on the development of generic formulations.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 2","pages":" 333-343"},"PeriodicalIF":0.0,"publicationDate":"2024-04-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/pm/d3pm00058c?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141424767","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}