Journal of microencapsulation最新文献

Oral administration of Propranolol suffers from lower bioavailability due to high hepatic first pass metabolism. The study undertakes development of propranolol loaded polymeric nanoparticles, that was further loaded into gel matrix for topical application. The nanoparticles were prepared by precipitation-ultra-sonication method and were assessed for their physico chemical properties, morphology, drug release, and permeation analysis. The propranolol loaded nanoparticles had a particle size of 123 nm with polydispersity index of 0.111. The entrapment efficiency of nanoparticles was 85% with percentage yield of 67%. The SEM study showed particles size in the range of 115 nm to 150 nm with smooth & spherical surface morphology. The XRD analysis revealed that nanoparticles were amorphous in nature. The nanoparticles loaded gel have optimum pH, viscosity and spreadability for topical application. The gel matrix showed 83% propranolol release within 24 hours and followed Higuchi model. The permeation of drug from the gel was higher at skin pH of 5.5, depicting the suitability of fabricated gel for potential application in Infantile Haemangiomas.

This study aims to study the combined anti-cancer effects of Simvastatin (SIM) and Thymoquinone (THY) against breast cancer cell lines and to develop and evaluate nanostructured lipid carriers (NLCs) encapsulating Simvastatin and Thymoquinone. Nanostructured lipid carriers (NLCs) co-loaded with Simvastatin and Thymoquinone were successfully formulated for enhanced anticancer activity. The formulations were characterised using Transmission Electron Microscopy (TEM), Scanning Electron Microscopy (SEM), and X-Ray Diffraction (XRD) to determine particle morphology and crystallinity. Key physicochemical parameters, including mean particle size, polydispersity index (PDI), zeta potential, and drug loading capacity, were systematically evaluated. Encapsulation efficiency and in vitro drug release profiles were assessed using the dialysis bag diffusion method, while formulation stability was monitored at 4 °C, 25 °C, and 40 °C over a defined period. In vitro biological evaluations were conducted on MCF-7 and MDA-MB-231 breast cancer cell lines. Cytotoxic potential was determined through MTT assay and IC50 value estimation. Cellular uptake was visualised using fluorescence microscopy, and apoptosis induction was quantified via flow cytometry using Annexin V-FITC/PI dual staining. The results suggest that the co-delivery of Simvastatin and Thymoquinone via NLCs enhances intracellular drug accumulation and promotes apoptosis, highlighting their potential as a synergistic nanocarrier-based therapy for breast cancer treatment. The optimised SIM-THY-NLCs were spherical with mean diameter of 105.6 ± 4.2 nm, PDI of 0.214 ± 0.03, and zeta potential of -28.6 ± 2.1 mV. Encapsulation efficiencies were 89 ± 1.59% (SIM) and 91 ± 1.45% (THY). Sustained drug release over 24 h was observed (SIM: 40%, THY: 65%). The NLCs showed significantly improved cytotoxicity with IC₅₀ values of 2.56 µg/ml (MCF-7) and 1.23 µg/ml (MDA-MB-231), alongside enhanced cellular uptake and apoptosis. SIM-THY-NLCs significantly improve drug stability, release, and anticancer efficacy on breast cancer cells establishing them as a promising nanocarrier system for effective breast cancer therapy.

Aim: The study reported development of Curcuma caesia leaf essential oil encapsulated poly(lactic-co-glycolic acid) (PLGA) nanocarrier-embedded gel as a potential strategy to treat periodontal infection.

Method: Curcuma caesia oil loaded experimental nanocarriers (CNCs) were developed by nano precipitation method and characterized. In vitro and in vivo efficacy of CNCs loaded gel (CNCsG) was evaluated.

Results: GC/MS analysis revealed Borneol as the major phytoactive constituent. CNCs were spherical, nanosized (51.28 ± 2.1 nm), with -40.5 ± 0.8% mV surface charge, 20.8 ± 0.7% w/w oil loading and 86.4 ± 1.3% encapsulation efficiency. CNCsG was reported with satisfied mucoadhesion (45.66 ± 2.2 dyne/cm2), viscosity (37745 ± 32.7 cps), spreadability (6.5 ± 1.2 gm.cm/sec), sustained ex-vivo release. A faster recovery of infection towards normal was observed in periodontitis rats by CNCsG than Clorni gel. Improved plasma pharmacokinetic profile was reported for CNCsG as compared to standard gel.

Conclusion: CNCsG was reported having promising antibacterial potency. In vivo efficacy data would lay foundation for futuristic clinical testing of CNCsG in periodontitis.

Context: Probiotic microencapsulation is an advanced technique designed to protect live probiotic microorganisms by enclosing them within a protective matrix, typically composed of biocompatible biopolymers.

Objective: This review provides a comprehensive analysis of recent advancements in bio-polymer coatings for probiotic microencapsulation, with a focus on chitosan and its synergistic combinations with other materials.

Methods: This methods highlights the necessity for continued innovation in bio-polymer coatings, emphasizing the development of bio-responsive materials, AI-driven formulation strategies, and next-generation encapsulation technologies to meet the evolving demands of functional foods and precision therapeutics.

Results: Probiotic microencapsulation plays a critical role in protecting probiotics from environmental stresses, improving stability, and ensuring targeted delivery. Innovations in chitosan-based encapsulation, including its combination with bio-polymers such as alginate, gelatin, and pectin, have enhanced encapsulation efficiency, controlled release, and probiotic viability. Cutting-edge techniques such as nanotechnology, stimuli-responsive coatings, and hybrid bio-polymers are explored for their potential to optimize probiotic performance in food and pharmaceutical applications.

Conclusions: Despite these advancements, obstacles remain in ensuring consistent release profiles, mitigating the inhibitory effects of chitosan on certain probiotic strains, and optimizing large-scale production while maintaining cost-effectiveness. The need for personalized probiotic therapies has driven research into adaptive encapsulation systems tailored to individual gut microbiota compositions.

Aim: To develop polyelectrolyte multilayer capsules (PMC) loaded with doxorubicin (DOX) and modified with the DR5-B protein to overcome drug resistance in MCF-7 breast cancer cells.

Methods: The capsules were prepared by layer-by-layer (LbL) assembly followed by thermal shrinking, DOX encapsulation and DR5-B surface modification. The capsules were characterised using scanning electron microscopy (SEM), dynamic light scattering (DLS), and UV-Vis spectrophotometry. Cellular uptake was assessed by confocal microscopy, flow cytometry, and fluorimetry. Cytotoxicity was evaluated by MTT-test in 2D and 3D in vitro models.

Results: Mean capsule size was 320 ± 90 nm (PDI 0.39), mean ζ-potential was +29 ± 5 mV. The encapsulation efficiencies (ЕЕ) of DOX and DR5-B were 85 ± 7% and 80 ± 4%, with loading capacities (LC) of 9 ± 2 w/w% and 145 ± 40 w/w%, respectively. Shrunken capsules exhibited 3.5-fold higher internalisation than non-shrunken ones. DR5-B increased capsule accumulation by 1.8-fold. The capsules showed synergistic cytotoxicity in DR5-B-resistant MCF-7 spheroids (IC50 227 ± 13 ng/mL), being non-toxic to fibroblasts.

Nanoemulsion (NE) is a kinetically stable dispersion comprising oil and water stabilised by an emulsifier, having a droplet size of around 20-200 nm. NE offers versatile formulations for lipophilic and hydrophilic drugs by increasing their solubility and permeability thereby improving their bioavailability. Various high energy and low energy techniques such as the phase pH inversion method, solvent diffusion method, and membrane emulsification method are reported to develop NE. The selection of method is crucial, thus a comparison of different methods in terms of droplet size and stability has been provided. This review emphasises the topical application of NE for various skin ailments like psoriasis, skin infection, cancer, wound healing, and many others. This review highlights the advancement in the NE formulation using ionic liquids and nanoparticles, as well as stimuli-responsive and pickering NE. The approaches to overcome the toxicity concern of NE and its constituents specifically surfactant has been discussed.

Aims: To develop and evaluate a biocompatible, stable, ultrasound-responsive hybrid nanocarrier for effective therapeutic outcomes.

Methods: The hybrid liposome-polymer drug delivery system (hLPDS) was characterised using dynamic light scattering, photoluminescence, atomic force microscopy, Raman spectroscopy and evaluated for drug release, cytotoxicity, cell uptake, and biodistribution.

Results: The hLPDS demonstrated mean diameter of 120 ± 5 nm and polydispersity index of 0.58 ± 0.83, zeta potential of 30 ± 5 mV, encapsulation efficiency of 93 ± 2.9%, loading capacity of 13 ± 1.5% (w/w) and remained stable for 90 days. The hLPDS showed 10% cell viability and lower IC₅₀ (1.274 ± 0.32 µM) compared to free drug (1.842 ± 0.32 µM). Ultrasound at 4 MHz frequency increased drug release above 90% (w/v), enhanced cellular internalisation (p < 0.0001), and anti-proliferative effects.

Conclusion: Ultrasound-triggered hLPDS exhibited enhanced cytotoxicity, cell uptake, stability, and therapeutic effect compared to liposomes and micelles alone.

To enhance the antioxidant properties of unsaturated fatty acids (UFAs), a UFAs microemulsion (UFAs-M) is prepared via direct emulsification. Its storage stability is evaluated using laser diffraction, while the antioxidant properties of both UFAs-M and free UFAs are assessed using the DPPH method. The effects of temperature and UV exposure are also investigated. Over a 90-day period, the mean particle diameter of UFAs-M ranges from 49.1 nm to 57.4 nm, with zeta potential values between -11.79 mV and -13.13 mV. The polydispersity index (PDI) ranges from 0.276 ± 0.045 to 0.319 ± 0.049. The encapsulation efficiency varies from 98.4 ± 0.59% (w/w) to 91.5 ± 0.98% (w/w), and the drug loading ranges from 0.984 ± 0.011% (w/w) to 0.862 ± 0.013% (w/w). The DPPH radical scavenging activity of UFAs-M (82.8 ± 3.15%) is significantly higher than that of UFAs (65.33 ± 0.26%). Moreover, UFAs-M exhibits superior antioxidant performance under high temperature and UV exposure. Overall, the microemulsion system enhances both the antioxidant capacity and storage stability of UFAs, showing promising potential for practical applications.

Approximately 90% of drugs struggle with low solubility and non-selectivity in target-specific drug delivery. This creates a significant challenge due to the limited permeability of the blood-brain barrier (BBB) and blood-cerebrospinal fluid (CSF) barrier. Poor solubility, low drug concentration at the target site, and rapid clearance via efflux transporters further restrict effective drug delivery in neurodegenerative disorders (NDDs). Nanocrystal (NC) technology offers a promising approach by producing sub-micron, carrier-free NCs with high drug payload, stabilised with stabilisers to enhance colloidal stability and shelf life. The increased surface area boosts the solubility, bioavailability, and brain permeability of hydrophobic drugs, making NCs an emerging technology for both therapeutic and diagnostic applications in neurodegenerative diseases. NCs are synthesised via top-down, bottom-up, and combinational methods, with NANOEDGE^® and SmartCrystals^® being some of the patented technologies. Despite the high potential of NCs in improving drug delivery to the brain, many challenges remain, including thermal instability, scalability, and long-term safety.

Aim: To develop and optimise a niosomal formulation of ulipristal acetate (UPA) for enhanced cytotoxicity against uterine fibroids.

Methods: Quality by Design, thin film hydration, dynamic light scattering, transmission electron microscopy, cytotoxicity assays, flow cytometry, reactive oxygen species (ROS) generation analysis.

Results: Optimised UPA-loaded niosomes (UPA-NS) exhibited mean diameter of 170.7 ± 3.46 nm, polydispersity index of 0.23 ± 0.02, zeta potential of -18.2 ± 2.31 mV, encapsulation efficiency of 90.57 ± 3.22%w/w and 10.65 ± 1.64%w/w loading efficiency. UPA-NS showed 89 ± 3.22%w/w drug release at pH 5.5 within 24 hours compared to 36 ± 5.44%w/w at pH 7.4. UPA-NS demonstrated 70% cytotoxicity in HEC-6 cells at 0.5 μg/mL compared to 44% for free UPA. Flow cytometry showed 23% live cells for UPA-NS vs 33% for free UPA after 16 hours. UPA-NS induced higher ROS generation than free UPA.

Conclusions: The niosomal formulation enhanced the cytotoxicity and ROS-generating potential of UPA against uterine fibroid cells.