JOURNAL OF MICROENCAPSULATION

Advancements in microneedle technology: current status and next-generation innovations
Kumar S and Shukla R
Microneedle technology is a pivotal component of third-generation transdermal drug delivery systems featuring tiny needles that create temporary microscopic channels in the stratum corneum which facilitate drug penetration in the dermis. This review offers a detailed examination of the current types of microneedles, including solid, coated, dissolving, hollow, and swelling microneedles, along with their preparation techniques as well as their benefits and challenges. Use of 3D printing technology is especially gaining significant attention due to its ability to achieve the high dimensional accuracy required for precise fabrication. Additionally, its customisability presents significant potential for exploring new designs and creating personalised microneedles products. Furthermore, this review explores next generation microneedles, especially stimuli-responsive microneedle, bioinspired microneedle and microneedles combined with other transdermal technology like sonophoresis, electroporation and iontophoresis. Regulatory aspects, characterisation techniques, safety considerations, and cost factors have also been addressed which are crucial for translation from lab to the market.
Effect of poly(ε-caprolactone) microspheres on population pharmacokinetic/pharmacodynamic model of a simple coumarin
Cárdenas PA, Alves IA, De Araujo BV and Aragón DM
This study aims to evaluated the impact of poly(ε-caprolactone) (PCL) microspheres on the pharmacokinetics and pharmacodynamics (PopPK/PD) of 6-methylcoumarin (6MC). For this, PCL microspheres loaded with 6MC were prepared using the emulsification-evaporation method. Particle size, zeta potential, drug loading, and entrapment efficiency were characterised by dynamic light scattering and UV spectrophotometry. In vitro release and pharmacokinetics in Wistar rats were assessed for free and encapsulated 6MC. Anti-inflammatory activity was evaluated using the carrageenan-induced paw edoema model, with PopPK and PopPK/PD models developed. Microspheres showed diameters between 2.9 and 7.1 µm, zeta potentials of -10 to -15 mV, and drug loading of 0.24 mg/mg. Encapsulation efficiency was 45.5% to 75.9%. PopPK models showed enhanced absorption and distribution, with increased anti-inflammatory potency of encapsulated 6MC. PCL microspheres significantly improved the pharmacokinetic and pharmacodynamic profiles of 6MC, enhancing its therapeutic potential for lipophilic drugs.
A comprehensive review on lipid-based nanoparticles via nose to brain targeting as a novel approach
Hameed H, Faheem S, Younas K, Jamshaid M, Ereej N, Hameed A, Munir R and Khokhar R
The central nervous system (CNS) has been a chief concern for millions of people worldwide, and many therapeutic medications are unable to penetrate the blood-brain barrier. Advancements in nanotechnology have enabled safe, effective, and precise delivery of medications towards specific brain regions by utilising a nose-to-brain targeting route. This method reduces adverse effects, increases medication bioavailability, and facilitates mucociliary clearance while promoting accumulation of drug in the targeted brain region. Recent developments in lipid-based nanoparticles, for instance solid lipid nanoparticles (SLNs), liposomes, nanoemulsions, and nano-structured lipid carriers have been explored. SLNs are currently the most promising drug carrier system because of their capability of transporting drugs across the blood-brain barrier at the intended brain site. This approach offers higher efficacy, controlled drug delivery, target specificity, longer circulation time, and a reduction in toxicity through a biomimetic mechanism.
Biodegradable polymeric nanocomposite containing phloretin for enhanced oral bioavailability and improved myocardial ischaemic recovery
Sharma P, Bal T, Singh SK and Sharma N
The study aimed to enhance phloretin's oral absorption and systemic availability through nanoencapsulation within biodegradable polymers, improving its anti-oxidant and cardioprotective potential.
Leflunomide nanocarriers: a new prospect of therapeutic applications
Zewail M
Leflunomide (LEF) is a well-known disease-modifying anti-rheumatic agent (DMARDs) that was approved in 1998 for rheumatoid arthritis (RA) management. It is enzymatically converted into active metabolite teriflunomide (TER) inside the body. LEF and TER possess several pharmacological effects in a variety of diseases including multiple sclerosis, cancer, viral infections and neurobehavioral brain disorders. Despite the aforementioned pharmacological effects exploring these effects in nanomedicine applications has been focused mainly on RA and cancer treatment. This review summarises the main pharmacological, and pharmacokinetic effects of LEF along with highlighting the applications of nanoencapsulation of LEF and its metabolite in different diseases.
Dermal drug delivery bilosomes: a synergistic integration for better therapeutic outcomes
Aralelimath K, Sahoo J and Wairkar S
The dermal route is commonly used to deliver the drugs at the targeted site and achieve maximum therapeutic efficacy. The stratum corneum, the uppermost layer of the skin, presents a significant diffusional barrier for most drugs. Various nanoformulations face challenges such as limited drug absorption and inadequate retention at the targeted site, frequently hindering therapeutic efficacy. Researchers are increasingly exploring innovative strategies that leverage nanotechnology and specialized carriers to address these challenges and enhance the outcomes of dermal medications. A novel drug delivery system, bilosomes, has been designed as a potential vesicular carrier system for the dermal route. Bilosomes are colloidal, lipid-based vesicles stabilized with bile salts, offering greater stability during storage and transportation. The lipid bilayer of bilosomes imparts ultra-flexibility, facilitating penetration through the stratum corneum. This review explores the use of bilosomes in dermal formulations for treating diverse diseases, their developmental techniques, and characterization, and it sheds light on their advantages over traditional lipid nanocarriers.
Physicochemical stability and controlled release of vitamin D-loaded emulsions stabilised by whey protein isolate-basil seed gum conjugates
Kouravand F, Shahidi F, Fathi M, Koocheki A and Roshanak S
The present study was conducted to produce a new carrier containing whey protein isolate-basil seed gum (WPI-BSG) conjugate to achieve superior physicochemical stability of emulsions containing vitamin D (Vit-D).
A comparative analysis of PLA and PCL microparticles for hydrophilic and hydrophobic drugs
Panigrahi SK, Das S and Majumdar S
This study aims to investigate Polylactic Acid (PLA) and Polycaprolactone (PCL) polymers for microencapsulation of hydrophilic and hydrophobic anti-glaucoma drugs using an emulsion-based solvent evaporation technique. Microparticle size was analysed using optical microscopy, while drug-polymer interactions through Dynamic-Light-Scattering (DLS) and Fourier-Transform-Infra-red/Attenuated-Total-Reflection spectroscopy (FTIR/ATR). , drug release studies were performed to investigate drug encapsulation and release profiles. Spherical microparticles, with particle size 94 ± 6.9 μm for PCL-based and 100 ± 3.74 μm for PLA-based formulation, were obtained. Drug release studies showed 100% release over about 32 days, with encapsulation efficiency (%EE) and drug loading (%w/w) reaching up to 95 and 2.84% for PLA-based and 97 and 2.91% for PCL-based microparticles, respectively. DLS studies reveal an increase in hydrodynamic radius (), which correlates to enhanced drug encapsulation. So, the nature of the drug and polymer significantly impacts drug encapsulation and release, with drug-polymer interactions playing a crucial role alongside experimental parameters.
Synthesis of cefixime loaded PCL/HPMC blend nanoparticles: a controlled release study and anti-bacterial evaluation
Naik Y, Naik HN, Rai J, Shah R, Jauhari S and Patel AJ
To enhance cefixime's effectiveness and address drug delivery challenges like concentration at the site, dose, and time, present study investigated the impact of polymer blends on cefixime's release profile.
Paliperidone-loaded nose to brain targeted NLCS: optimisation, evaluation, histopathology and pharmacokinetic estimation for schizophernia
Khedkar MA, Sharma V, Anjum M, Singh S, Shah K, Alam P and Dewangan HK
Study was to develop a nanostructured-lipid-careers (NLCs) of paliperidone (PLP) for nose-to-brain targeting. NLCs was prepared by sonication, high-shear homogenisation method, and characterised their mean diameter, PDI, zeta-potential, morphology (by SEM, TEM and AFM), entrapment efficiency, drug loading, release, interaction study (by FTIR), and stability. Further, permeation and ciliotoxicity performed in sheep nasal mucosa, and biodistribution/pharmacokinetic was performed in rats for schizophernia. Developed NLCs showed spherical and clearly 3-dimentinal structure with 129 ± 2.7 nm mean diameter, 0.304 ± 0.003 PDI, -7.61 ± 0.56 mV zeta-potential, 58.16 ± 0.17% entrapment efficiency, 65.8 ± 2% drug loading and 74.32 ± 0.003% release in 12 h, followed by Higuchi model. study showed NLCs have three times higher permeation, compare to pure drug (around 71.50.32% in 6 h) and 3.98 g/cm/h steady sate flux. The blood/brain ratio given by intranasally have higher compare to IV route, and 94.53 ± 21.45% drug targeting efficiency in brain. In conclusion, NLCs have easily crossed BBB, higher drug delivery and effective for schizophrenia in given by intranasal.
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The assessment of pharmacokinetics and neuroprotective effect of berberine hydrochloride-embedded albumin nanoparticles via various administration routes: comparative studies in rats
Attia HG, Elmataeeshy ME, Aleraky M, Saleh SR, Ghareeb DA, El Demellawy MA, El-Nahas HM and Ibrahim TM
The current study aimed to evaluate the pharmacokinetics and neuroprotective effect of well-characterised berberine-bovine serum albumin (BBR-BSA) nanoparticles. BBR-BSA nanoparticles were generated by desolvation method. Entrapment efficiency, loading capacity, particle size, polydispersity index, surface morphology, thermal stability, and release were estimated. pharmacokinetic and tissue distribution were conducted. Their neuroprotection was evaluated against lipopolysaccharides-induced neurodegeneration. BBR-BSA nanoparticles showed satisfactory particle size (202.60 ± 1.20 nm) and entrapment efficiency (57.00 ± 1.56%). Results confirmed the formation of spheroid-thermal stable nanoparticles with a sustained drug release over 48 h. Sublingual and intranasal routes had higher pharmacokinetic plasma profiles than other routes, with C values at 0.75 h (444 ± 77.79 and 259 ± 42.41 ng/mL, respectively). BBR and its metabolite distribution in the liver and kidney were higher than in plasma. Intranasal and sublingual treatment improves antioxidants, proinflammatory, amyloidogenic biomarkers, and brain architecture, protecting the brain. In conclusion, neuroinflammation and neurodegeneration may be prevented by intranasal and sublingual BBR-BSA nanoparticles.
Interactions of human serum albumin with phosphate and Tris buffers: impact on paclitaxel binding and nanoparticles self-assembly
Gonzalez-Posada AH, Mesa M, Sierra L and Lopez B
To investigate the conformational changes in human serum albumin (HSA) caused by chemical (CD) and thermal denaturation (TD) at pH 7.4 and 9.9, crucial for designing controlled drug delivery systems with paclitaxel (PTX).
Preparation of double-loaded bitter ginseng derivative B21-DOX liposomes co-modified with SP94 and BR2 ligand and its in vitro anti-hepatocarcinogenic effect
Jing L, Zhang J, Li L, Luo S, Tang Z, Liu X, Zhong Y and Yuan M
To construct a novel liposomal drug delivery system co-modified with SP94 and BR2 ligands, encapsulating both the bitter ginseng derivative B21 and doxorubicin (DOX), to achieve superior anti-tumour efficacy and reduced toxic side effects.
Development, QbD-based optimisation, pharmacokinetics, and evaluation of Eudragit RS 100 loaded flurbiprofen nanoparticles for oral drug delivery
Mandpe S, Kole E, Parate V, Chatterjee A, Mujumdar A and Naik J
This study aims to develop and evaluate flurbiprofen-loaded polymeric nanoparticles to achieve sustained drug release, enhancing therapeutic efficacy and minimising dosing frequency for improved patient outcomes. Flurbiprofen-loaded polymeric nanoparticles were prepared using a tubular microreactor and spray drying, optimised via Box-Behnken Design. Characterisation included particle size, encapsulation efficiency, in vitro and in vivo drug release, and techniques like FTIR, DSC, XRD, and SEM. Statistical analysis ensured robust formulation optimisation and evaluation of performance. The optimised batch of flurbiprofen-loaded polymeric nanoparticles was characterised for mean diameter, PDI, zeta potential, drug release, and EE% were found to be 306.1 ± 6.00 nm, 0.184 ± 0.02 Mw, -23.6 ± 1.51 mV, 85.46 ± 0.53% and 92.31 ± 0.84 (% w/w) respectively. Pharmacokinetic analysis further confirmed the sustained release, extending up to 12 hours and enhancing permeation compared to the pure flurbiprofen. Sustained release of flurbiprofen-loaded polymeric nanoparticles significantly enhances therapeutic effectiveness for inflammatory conditions.
Synergistic enhancement of chlorophenols removal using eco-friendly alginate@montmorillonite hybrid bio-capsules: insights from encapsulation and kinetic release studies
Essifi K, Brahmi M, Boussetta A, Charii H, Ait Benhamou A, El Bachiri A, Salhi S, Brahmi R, Moubarik A and Tahani A
This study investigates the synergistic effects of alginate@montmorillonite (Alg@Mt) hybrid microcapsules for enhancing water purification, focusing on improving the encapsulation of hydrophobic contaminants. Alg@Mt microcapsules were prepared through ionotropic gelation. Characterisation was performed using SEM-EDX, FTIR, XRD, and TGA. Encapsulation efficiency (EE), loading capacity (LC), and release behaviour were also examined. Alg@Mt microcapsules effectively removed phenol and its chlorinated derivatives from water. Incorporating Na-Mt improved structural and thermal properties, EE, and LC. Increasing the clay content to 60% (w/w) raised the EE of phenol and its more hydrophobic derivative, 2,4,6-trichlorophenol, from 39.74 ± 3.1% (w/w) and 63.91 ± 2% (w/w) to 60.56 ± 1.6% (w/w) and 82.28 ± 2.3% (w/w), respectively, with more controlled release rates, following Fickian diffusion mechanism. EE increased with phenolic substances hydrophobicity, while LC and release rates were inversely related. This approach is promising for removing hydrophobic contaminants from water.
Recent updates of carotenoid encapsulation by spray-drying technique
Griep P, Gayeski L, Colet R, Zeni J and Valduga E
Carotenoids are compounds sensitive to environmental factors such as light, heat, and oxygen, which can result in the loss of their properties due to isomerisation and oxidation. To overcome this problem, spray drying encapsulation has been widely used as a method to protect and stabilise carotenoids in different wall materials. This article summarises the findings and research on spray drying encapsulation of carotenoids over the past 15 years, with an emphasis on the importance of controlling the operational conditions of the drying process and the association of different wall materials (proteins and polysaccharides), promising to increase encapsulation efficiency and stabilise carotenoids, with perspectives and trends in applications. The use of spray drying for carotenoid microencapsulation can open up new opportunities for controlled delivery of beneficial compounds. Based on the study, it is expected to provide information for researchers, professionals, and companies interested in the development of functional food products.
Nanoparticles encapsulated in polysaccharide-based pellets as colon targeting approach
Arora A, Sharma A, Singh S, Singh R, Singh A, Kakkar D and Sharma N
This article explores the application of mesalazine-loaded nanoparticles (MLZ-NPs) encapsulated in plant polysaccharide-based pellets (MLZ-NPs-Pellets) for ulcerative colitis.
Spray-dried chitosan oligosaccharide microparticles with polyvinyl alcohol-based dispersions for improved gefitinib solubility
Ahir SB, Vallamkonda B, Reddy Challa R, Chopade N, Deshmukh PK and More MP
The aim of research is to enhance the solubility of crystalline gefitinib (GF), a poorly water-soluble drug, by developing drug delivery systems using chitosan oligosaccharide (COS) particle engineering. Fabrication utilizes ionic gelation followed by spray drying. The preliminary evaluations such as Uv-Vis, FTIR, DSC followed by advanced techniques like SEM and invitro drug release characteristics was performed along with solubility study. The spray-dried particles measured a mean diameter of 3.18 ± 0.5 microns, %EE as well as load w/w improved from 63.25 ± 2.1% and 37.98 ± 1.5% w/w (COS nanoparticles) to 78.15 ± 2.6% and 45.34 ± 1.6% w/w (engineered microparticles), respectively. The zeta potential and in vitro studies demonstrated 41 ± 3.5 mV and 92 ± 2.1% (w/w) release suggest long-term stability and prolonged release. This novel engineering approach effectively enhances GF solubility and surface characteristics, offering promising potential for improving delivery characteristics.
The potential of turmeric extract-loaded chitosan microparticles for the treatment of gastrointestinal disorders
Mittraparp-Arthorn P, Ungphaiboon S, Takahashi Yupanqui C, Suwannasin S, Wijukkul C, Tanmanee N and Srichana T
To develop turmeric extract-loaded chitosan microparticles for treating gastrointestinal disorders.
Lipid nanocarrier-based bigel of oil for analgesic and anti-inflammatory applications
Satapathy BS, Mishra A, Mohanty K, Pattnaik S, Tripathy S and Biswal B
Present study reports analgesic and anti-inflammatory potential of (L.) leaf oil loaded lipid nanocarrier (BLNs)-embedded bigel. BLNs were developed by solvent evaporation technique and were characterised by FESEM, Cryo-TEM, mean diameter, zeta potential, loading efficiency, etc. BLNs embedded bigel (BLNs-G) was evaluated for analgesic and anti-inflammatory efficacy in rat model. Data showed spherical BLNs with intact lamellarity, 138.2 ± 1.08 nm mean diameter, 0.182 PDI, -46.6 ± 0.61 mV zeta potential, 76.2 ± 2.1% (w/w) loading efficiency and a sustained release . BLNs-G was homogenous with satisfied viscosity (40 734 ± 1.7 cps), spreadability (8.3 ± 1.5 g.cm sec), extrudability (91.33 ± 1.3% w/w) along with a sustained permeation . Significant analgesic and anti-inflammatory action were depicted by BLNs-G (1% w/w) in rat model (p ˂ 0.05) within 30 minutes post topical application. docking study revealed high affinity of major phytoactive components with key analgesic/inflammatory mediators. Further pre-clinical investigations are warranted for futuristic clinical application of BLNs-G.