Osteoarthritis is associated with a weakly acidic intra-articular microenvironment, which provides an intrinsic trigger for pH-responsive drug delivery systems to achieve site-specific and controlled drug release, thereby enhancing therapeutic efficacy. In this study, celecoxib (CXB)-loaded microspheres (CM-10) for intra-articular injection were fabricated using a microfluidic technique with poly(lactic-co-glycolic acid) (PLGA)/CaCO₃ as the carrier. The microspheres were systematically characterized in terms of morphology, encapsulation efficiency, and physicochemical properties. Their pH-responsive drug release and degradation behaviors were evaluated under different in vitro conditions, and the degradation behavior following intra-articular injection was further investigated. In addition, the pharmacodynamic effects of CM-10 were assessed in an osteoarthritis model. The results demonstrated that CM-10 exhibited pronounced pH-responsive release, with accelerated drug release under acidic conditions and sustained degradation following intra-articular administration. Furthermore, CM-10 effectively promoted articular cartilage repair and improved therapeutic outcomes. These findings indicate that CM-10 has promising potential as a pH-responsive intra-articular drug delivery system for osteoarthritis therapy.

Poly (lactic-co-glycolic acid) (PLGA) microspheres are widely used for controlled drug delivery, but the drug existing state in the microspheres significantly influences the characteristics of microspheres. The focus of the present study was to formulate meloxicam injectable sustained release microspheres (MLX-MS) and to investigate the influence of the drug existing state within the microspheres on the release properties, degradation and to evaluate the intra-articular (IA) treatment efficacy of osteoarthritis (OA). Different MLX-MS were prepared by changing drug existing forms (microcrystal, particle and molecular state) by the method of cosolvent combination or micronized drug and they were characterized by scanning electron microscopy-energy dispersive spectroscopy (SEM-EDS), X-ray diffraction (XRD) and in vitro release. The therapeutic effect of MLX-MS was investigated using OA rabbits after IA injection. The degradation, drug retention, and pharmacodynamics were also assessed. The results highlighted that the release and degradation of MLX-MS in the joint cavity were directly correlated to the drug existing state. This study offers crucial insights for developing sustained-release injectable MLX-MS, the microspheres with drug existing in molecular state (Mol-MS) were the optimum formulation which can provide sustained release and more effective therapy of joint inflammation.

In this study, triamcinolone acetonide sustained-release microspheres (TrA-MS) were prepared by microfluidic method for intra-articular (IA) administration. The morphology, encapsulation efficiency, in vitro release and degradation of TrA-MS were characterized. The pharmacokinetics and pharmacodynamics of TrA-MS were investigated using papain-induced osteoarthritis (OA) rabbit models after IA injection. The results revealed that TrA-MS could achieve differential sustained release in the joint cavity. The pharmacokinetic curve in the joint fluid showed a synchronous TrA release trend with the plasma TrA curve. The data demonstrated a strong positive correlation between the released TrA from different TrA-MS in the joint cavity and the AUCs in both synovial fluid and plasma, and a highly significant correlation was also observed between the AUCs in the joint fluid and plasma. TrA-MS-755S demonstrated superior therapeutic efficacy, significantly delaying OA progression. In summary, TrA-MS prolonged drug release in the joint, inhibited inflammation progression, demonstrated the therapeutic advantage for OA therapy.

In this study, celecoxib (CXB) microspheres (CM) and ropivacaine (RPV) microspheres (RM) were prepared respectively. A poly (D, L-lactide-co-glycolide)-block-poly (ethylene glycol)-block-poly (D, L-lactide-co-glycolide) (PLGA–PEG–PLGA, PPP) was synthesized by copolymerizing glycolide and lactide with polyethylene glycol. CM, RM, and hydroxyapatite (HA) were then incorporated into PPP solution to construct the microsphere–hydrogel system (CRMH hydrogels). CM, RM, and CRMH were systematically characterized in terms of morphology, physicochemical properties, pH-buffering capacity, and degradation behavior. The pH-dependent drug release and release kinetics of the individual CM, RM and the CRMH hydrogels were also investigated. In vitro release studies demonstrated that CRMH hydrogels provided coordinated, sustained release of CXB and RPV at pH 6.2. In a rabbit osteoarthritis (OA) model, intra-articular (IA) administration of CRMH hydrogels achieved sustained drug retention and release within the joint cavity, and effectively promoted articular cartilage repair. Overall, the CRMH hydrogels showed promising synergistic therapeutic potential for OA.

This paper proposes a novel and efficient centrifugal microfluidic technology to prepare risperidone-loaded poly(lactic-co-glycolic acid) (PLGA) microspheres (RIS-MS). The effects of key parameters, including PLGA concentration and type, microchannel inner diameter and centrifugal speed on particle size, morphology and drug release were evaluated and optimized. The in vivo pharmacokinetic study of RIS-MS was conducted in rabbits. The results demonstrated that RIS-MS could be produced from microchannels with inner diameters of 170-210 μm at a centrifugal speed of 400 revolutions per minute (rpm) when the PLGA content is 15 % or higher. The mean plasma concentration of RIS-MS was more stable and Cmax of RIS-MS was significantly lower than that of the suspension group, and the RIS-MS could maintain the release of RIS in rabbits for up to 42 days. This study provided pioneering ideas for developing microspheres using centrifugal microfluidic technology. The optimized RIS-MS can make excellent sustained release and have the potential for the long-acting therapy of schizophrenia.

This study introduces a novel injectable, dynamically crosslinked hydrogel composite delivery system, diacerein microspheres (DIA-MS) encapsulated within a hydrogel matrix (DIA-MS@gel), for the potential treatment of osteoarthritis (OA). DIA-MS was fabricated using a T-junction microfluidic device. The injectable hydrogel was synthesized through the reaction of oxidized hyaluronic acid (OHA), quaternized chitosan (QCS), and adipic acid dihydrazide (ADH). Subsequently, DIA-MS was encapsulated into the hydrogel to form the DIA-MS@gel composite. The DIA-MS@gel was characterized by morphology, swelling behavior, pH response, degradability, and drug release kinetics. In vitro experiments showed that DIA-MS@gel could effectively prolong the drug release time to 47 days and showed pH-responsive degradation behavior. In vivo studies in rabbits indicated that intra-articular (IA) injection of DIA-MS@gel facilitated articular cartilage repair. The DIA-MS@gel provided continuous drug release for over 31 days within the rabbit joint cavity, potentially reducing administration frequency, attenuating inflammation, and promoting bone tissue regeneration. Furthermore, the DIA-MS@gel exhibited excellent biocompatibility, suggesting its potential as a practical clinical approach for managing OA.

Lycopene is a promising biological functional component with various biological activities and excellent pharmacological activities. However, its low water solubility and stability lead to low oral bioavailability, which limits its edible and medicinal research. Then, it is necessary to explore effective methods to protect lycopene from destruction and further exploit its potential benefits. The absorption of lycopene in vivo is affected by solubility, stability, isomer type, emulsifying ability, difficulty in forming micelles in vivo, and interaction with food components. Emulsions, pickering emulsions, micelles, liposomes, bigels, beasds, solid dispersions, microcapsules, nanoparticles, electrospinning and other drug delivery systems can be used as good strategies to improve the stability and bioavailability of lycopene. In this paper, the absorption process of lycopene in vivo and the factors affecting its bioavailability were discussed, and the preparation strategies for improving the stability, bioavailability, and health benefits of lycopene were reviewed, to provide some clues and references for the full utilization of lycopene in the field of health. However, there are still various unresolved mysteries regarding the metabolism of lycopene. The safety and in vivo studies of various preparations should be further explored, and the above technologies also face the challenge of industrial production.

Most fruits and vegetables are susceptible to spoilage after harvest, the transportation and preservation conditions can further decrease the product quality. As one of the main food preservation technologies, edible films/coatings are made of eatable materials to form thin layers that can maintain food freshness during transport and storage. This review summarizes different films/coating materials, including proteins (soy, whey, wheat gluten, gelatin), polysaccharides (chitosan, starch, cellulose) and lipids. However, the films/coatings prepared by single material have many deficiencies which can be made up by the combination of composite films/coatings. Moreover, several prepared methods (electrospinning, casting, extrusion, dipping, fluidized-bed, spraying, panning) used for films/coatings are introduced. Finally, the application and future directions of films/coatings in the preservation of fruits, vegetables and other food products are also presented.

Lycopene, a popular antioxidant, exists abundantly in nature in all-E form, but the Z-lycopene has better solubility and absorption characteristics. Lycopene is labile to light, thermal and oxygen. Emerging technological approaches are developed to improve the stability of lycopene during production and processing. This review presents the degradation mechanism of lycopene. A comprehensive evaluation has made by comparing the advantages and disadvantages of different extraction and isomerization methods. Encapsulation of lycopene in different delivery systems can further improve its stability. The process and formulation influence factors, as well as the advantages and disadvantages of lycopene encapsulation delivery systems are summarized. In the future, it is necessary to scientifically design low-cost and high-efficiency lycopene production methods.The stable and high bioavailable lycopene encapsulation systems need to be designed. Further study on the chemical stability mechanism of lycopene, the toxicity of biological materials, the safety of lycopene preparations also need to be evaluated.

In this study, a new gastro-floating sustained-release capsule (GFC) with levodopa (LD) and benserazide hydrochloride (BH) was successfully developed. GFCs were prepared by filling the LD and BH granules into hard capsules and coated with cellulose acetate (CA) solution as a controlled-release layer. The effects of formulation factors on the release of GFCs were conducted. The AUC0 24 (µg h/mL) of LD were 69.31 ± 3.61 (μg h/mL) and 28.87 ± 2.58 (μg h/mL) and the Cmax were 7.84 ± 0.34 (μg/mL) and 9.21 ± 1.04 (μg/mL) in the GFCs and commercial tablets respectively. The relative bioavailability of LD was 267.55 ± 34.54

NanomedicineVol. 17, No. 18 EditorialEnhanced permeability and retention effect-focused tumor-targeted nanomedicines: latest trends, obstacles and future perspectiveSaurabh Shekhar‡, Mahima Chauhan‡, Sonali, Bhavna Yadav, Rohit Dutt, Liandong Hu, Madaswamy S Muthu & Rahul Pratap SinghSaurabh Shekhar‡ https://orcid.org/0000-0002-1320-3451Department of Pharmacy, School of Medical and Allied Sciences, GD Goenka University, Gurugram, 122103, India, Mahima Chauhan‡ https://orcid.org/0000-0003-2355-5511Department of Pharmacy, School of Medical and Allied Sciences, GD Goenka University, Gurugram, 122103, India, Sonali https://orcid.org/0000-0002-0111-7257Guru Teg Bahadur Hospital, GTB Enclave, Dilshad Garden, New Delhi, Delhi, 110095, India, Bhavna Yadav https://orcid.org/0000-0003-0242-5160Department of Pharmacy, School of Medical and Allied Sciences, GD Goenka University, Gurugram, 122103, India, Rohit Dutt https://orcid.org/0000-0001-6794-5533Department of Pharmacy, School of Medical and Allied Sciences, GD Goenka University, Gurugram, 122103, India, Liandong Hu https://orcid.org/0000-0002-9436-6913College of Quality and Technical Supervision and Key Laboratory of Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University, Baoding, 071002, China, Madaswamy S Muthu https://orcid.org/0000-0001-5805-7921Department of Pharmaceutical Engineering and Technology, Indian Institute of Technology (BHU), Varanasi, 221005, India & Rahul Pratap Singh *Author for correspondence: Tel.: +91 945 464 0967; E-mail Address: anuraza2009@gmail.comhttps://orcid.org/0000-0001-6807-0484Department of Pharmacy, School of Medical and Allied Sciences, GD Goenka University, Gurugram, 122103, IndiaPublished Online:22 Sep 2022https://doi.org/10.2217/nnm-2022-0065AboutSectionsView ArticleView Full TextPDF/EPUB ToolsAdd to favoritesDownload CitationsTrack CitationsPermissionsReprints ShareShare onFacebookTwitterLinkedInReddit View articleKeywords: cancer nanomedicinescancer/oncologycontrolled drug releaseenhanced permeability and retention effectfactors affecting EPR effectnanoparticle toxicitytargeted cancer therapyPapers of special note have been highlighted as: • of interest; •• of considerable interestReferences1. 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Nanomater. 19(2), (2012). •• Discusses the current benefits of using nanoparticle therapy in different types of cancer and highlights the importance of further studies regarding nanomaterial-induced toxicity.Google ScholarFiguresReferencesRelatedDetailsCited ByMicrowave triggered multifunctional nanoplatform for targeted photothermal-chemotherapy in castration-resistant prostate cancer27 February 2023 | Nano Research, Vol. 72RGD-decorated PLGA nanoparticles improved effectiveness and safety of cisplatin for lung cancer therapyInternational Journal of Pharmaceutics, Vol. 633 Vol. 17, No. 18 STAY CONNECTED Metrics Downloaded 33 times History Received 4 April 2022 Accepted 22 August 2022 Published online 22 September 2022 Published in print August 2022 Information© 2022 Future Medicine LtdKeywordscancer nanomedicinescancer/oncologycontrolled drug releaseenhanced permeability and retention effectfactors affecting EPR effectnanoparticle toxicitytargeted cancer therapyFinancial & competing interests disclosureAuthor R Pratap Singh acknowledges Science and Engineering Research Board, Department of Science and Technology, Ministry of Science and Technology, Government of India, for providing financial support (EEQ/2019/000218) under the scheme of Empowerment and Equity Opportunities for Excellence in Science. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.No writing assistance was utilized in the production of this manuscript.PDF download

The objective of this study was to explore an innovative sustained release technology and design a new microporous resin-based polymer device (RPD) for controlled release of glipizide (GZ). Photocurable resin was applied to prepare the resin layer to control GZ release. The impact of formulation parameters consisting of the type and amount of pore formers and pH modifiers, photocurable curing time as well as the weight of resin layer on GZ release were examined. The GZ-RPD was fabricated applying 24 mg of resin layer with PEG400 (100 % of the resin weight) as pore former and 10 mg of Na2CO3 as pH modifier. Scanning electron microscopy (SEM) demonstrated resin particles presenting a porous structure constituted the resin layer. The GZ-RPD possessed prolonged Tmax and reduced Cmax relative to commercial tablets. The relative bioavailability of the RPDs as well as commercial tablets was 93.65 % since the AUC0-24 h were 6111.05 +/- 238.89 ng.h/mL and 6525.09 +/- 760.59 ng h/mL, respectively. The release mechanism of the GZ-RPD was discussed. This paper provided an innovative concept to produce controlled GZ release oral formulation fabricated by photocurable resin, which demonstrated both excellent in vitro release and in vivo pharmacokinetics.

开发了一种适合肝动脉灌注化疗栓塞(TACE)用的姜黄素载药微球,并探究其对肝癌的治疗效果.以聚乙烯醇(PVA)为载体,采用乳液交联法制备微球,观察微球的外观和粒度,证明微球对癌细胞的抑制作用,在VX2兔模型中评估肝动脉栓塞微球治疗肝癌的功效.扫描电镜和粒度分析显示制备的微球球形完整;生物安全性证明微球材料安全指数较高;药效学研究表明姜黄素栓塞微球可在栓塞给药后有效发挥动脉栓塞作用,提高肝癌的治疗效果.本研究成功地制备了姜黄素栓塞微球,有望将其用于栓塞以提高TACE在肝癌中的治疗效果.

Arthritis is a kind of chronic disease that affects joints and muscles with the symptoms of joint pain, inflammation and limited movement of joints. Among various clinical therapies, drug therapy has been extensively applied because of its accessibility, safety and effectiveness. In recent years, the intra-articular injection has dramatic therapeutic effects in treating arthritis with high patient compliance and low side effects. In this review, we will introduce pathology of arthritis, along with the accessible treatment and diagnosis methods, then we will summarize major advances of current hopeful intra-articular delivery systems such as microspheres, hydrogels, nanoparticles and liposomes. At last, some safety assessments in the preclinical work and the main challenges for the further development of intra-articular treatment were also discussed.

Freeze-drying technology is an interdisciplinary and complex technology, combined with freezing and vacuum drying, It has become an important technology for heat-sensitive drugs and food preservation. Freeze-dried foods are classified into meat, vegetables, fruits, fungus, and micro-powders, etc. In this paper, the definition, principle, steps, advantages and disadvantages of freeze-drying are summarized, and the research progress of freeze-drying in food industry in recent years is reviewed, including the technological parameters and influencing factors.

Nutraceuticals have been gradually accepted as food ingredients that can offer health benefits and provide protection against several diseases. It is widely accepted due to potential nutritional benefits, safety, and therapeutic effects. Most nutraceuticals are vulnerable to the changes in the external environment, which leads to poor physical and chemical stability and absorption. Several researchers have designed various encapsulation technologies to promote the use of nutraceuticals. Microfluidic technology is an emerging approach which can be used for nutraceutical delivery with precise control. The delivery systems using microfluidic technology have obtained much interest in recent years. In this review article, we have summarized the recently introduced nutraceutical delivery platforms including emulsions, liposomes, microspheres, microgels, and polymer nanoparticles based on microfluidic techniques. Emphasis has been made to discuss the advantages, preparations, characterizations, and applications of nutraceutical delivery systems. Finally, the challenges, several up-scaling methods, and future expectations are discussed.

In the modern food industry, people are paying more and more attention to the use of edible nanoemulsions to encapsulate, protect and deliver lipophilic functional ingredients, such as volatile additives, polyphenols, aromas, pigments, proteins, vitamins, oil-soluble flavors, preservatives, etc., which are the current global needs. Nanoemulsions are constructed with droplets of nano range size and they offer many potential advantages over conventional emulsions including the delivery of both hydrophilic and hydrophobic compounds, higher stability, better antibacterial properties, good taste experience, higher affinity, longer shelf-life and improvement of the bioavailability of components. Moreover, they are highly capable of improving the wettability and/or solubility of poorly water-soluble compounds, which may result in better pharmacokinetic and pharmacodynamic properties of nutraceutical compounds. On the other hand, oral nanoemulsions also have certain risks, such as their ability to change the biological fate of biologically active ingredients in the gastrointestinal tract and the potential toxicity of certain ingredients used in their production. This review article summarizes the manufacturing, application, characterization, biological fate, potential toxicity, and future challenges and trends of nanoemulsions, and focuses on nanoemulsion-based nutraceutical delivery approaches suitable for the food industry.

Since last two decades, the controlled release systems have attracted more attention due to the several extraordinary features including better stability of the products and controlled drug release on followed by zero-order kinetics. Here, an advanced dental resin based controlled release system (DR-CRS) containing huperzine A (HupA) was developed to achieve a controlled drug release. The drug loaded tablet core was put into a polypropylene reservoir and then dental resin mixed with pore formers was coated on it as the controlled release layer. The effect of type and content of fillers, type and content of pore formers, and resin layer gain on the drug release was thoroughly investigated. The in-vitro drug release study showed that the optimized formulation had a total cumulative release of more than 95% in 8 h. The pharmacokinetic study revealed that the C-max value of DR-CRS was lower than that of the commercial tablets, the T-max value was prolonged, demonstrating the prominent controlled release performance of HupA. Furthermore, the DR-CRS with a relative bioavailability of 88.36% displayed good absorption. The advanced DR-CRS was capable of providing a satisfactory alternative to release the drug in a controlled manner, which would better meet the needs of the market and industrial production.

The aim of this study was to formulate osmotic pump capsules (OPCs) to control the release of nifedipine (NP). NP solid dispersion was prepared by solvent evaporation method. The prepared mixture of NP solid dispersion and various excipients were filled into the commercial HPMC hard capsule shells and then coated with cellulose acetate (CA) solution to form NP-OPC. The CA coating solution consisted of CA as semi-permeable membrane, and Poloxamer 188 as pore formers. The impact of addition agents, citric acid and pore formers on in vitro drug release were investigated. Furthermore, the study has highlighted the impact of paddle speed and the pH value of release media, on the release and compared the release with the commercial controlled release tablets. The in vitro drug release study indicated that drug release could reach 95% in 24 h with optimal formulation, and interestingly model fitting showed that the drug release behavior was closely followed to zero-order release kinetics. The pharmacokinetic studies were performed in rabbits with commercial controlled release tablets as reference, both preparations showed a sustained release effect. Compared with traditional preparation methods of OPCs, the new preparation process was simplified without the operation of laser drilling and the sealing process of capsule body and cap, which improved the feasibility of industrial production.

Due to special cavity structure, cyclodextrin can form inclusion complex with a large number of compounds, which can be widely used in food industry, such as enhancing antibacterial activity, extending the storage period of food, increasing the solubility of food ingredients, removing cholesterol in food and so on. In this paper, the formation mechanism, classification and properties of cyclodextrin inclusion complex were reviewed, and the applications of cyclodextrin and its derivatives in food industry were discussed.