Journal of microencapsulation最新文献

Aim: Our aim was to repurpose atorvastatin for melanoma by encapsulating in a nanostructured lipid carrier matrix to promote tumour cell internalisation and skin permeation. pH-responsive chitosan gel was employed to restrict At-NLCs in upper dermal layers.

Methods: We utilised a quality by design approach for encapsulating At within the NLC matrix. Further, cellular uptake and cytotoxicity was evaluated along with pH-responsive release and ex vivo skin permeation.

Results: Cytotoxicity assay showed 3.13-fold enhanced cytotoxicity on melanoma cells compared to plain drug with nuclear staining showing apoptotic markers. In vitro, release studies showed 5.9-fold rapid release in chitosan gel matrix at pH 5.5 compared to neutral pH.

Conclusions: At-NLCs prevented precipitation, promoted skin permeation, and SK-MEL 28 cell internalisation. The localisation of NLCs on the upper dermal layer due to electrostatic interactions of skin with chitosan gel diminished the incidence of untoward systemic effects.

Aim: This study aimed to prepare, characterise, and evaluate the antidiabetic activity of Coccinia grandis (L.) extracts encapsulated alginate nanoparticles.

Methods: Alginate nanoparticles were prepared using the ionic gelation method and characterised by encapsulation efficiency %w/w, loading capacity %w/w, particle size analysis, zeta potential, Fourier transform infra-red spectroscopy (FTIR), and scanning electron microscopy (SEM). In vitro antidiabetic activity was also evaluated.

Results: Encapsulation efficiency %w/w, loading capacity %w/w, mean diameter, zeta potential of C. grandis encapsulated alginate nanoparticles ranged from 10.51 ± 0.51 to 62.01 ± 1.28%w/w, 0.39 ± 0.04 to 3.12 ± 0.11%w/w, 191.9 ± 76.7 to 298.9 ± 89.6 nm, -21.3 ± 3.3 to -28.4 ± 3.4 mV, respectively. SEM and FTIR confirmed that particles were in nano range with spherical shape and successful encapsulation of plant extracts into an alginate matrix. The antidiabetic potential of aqueous extract of C. grandis encapsulated alginate nanoparticles (AqCG-ANP) exhibited inhibition in α-amylase, α-glucosidase and dipeptidyl peptidase IV enzymes of 60.8%c/c, 19.1%c/c, and 30.3%c/c, respectively, compared to the AqCG.

Conclusion: The AqCG-ANP exerted promising antidiabetic potential as an antidiabetic drug lead.

Aim: The goal of this study is to optimisation and evaluation of dopamine-loaded NLC (NLC-DOPA) for achieve dopamine concentrations into brain for treatment of Parkinson's disease which causes progressive neuronal death.

Method: NLC-DOPA prepared by homogenisation method using solid lipids (Cholesterol and Soya lecithin), liquid lipid (Oleic acid) and surfactant (Poloxamer- 188) as major excipients, optimised by central composite design using design expert-13 software. The optimised formulations were characterised by particle size, zeta potential, entrapment efficiency, SEM, TEM, FTIR, DSC, XRD, stability study and in-vitro drug release. The histopathology of rat brain tissues and goat nasal tissues were performed. The ex-vivo (permeability and nasal ciliotoxicity study) and in vivo pharmacodynamics study were also accomplished to determine its efficacy and potency of NLC.

Result: The NLC-DOPA formulations were optimised in particle size and (EE)% with range from 85.53 ± 0.703 to 106.11 ± 0.822 nm and 82.17 ± 0.794 to 95.45 ± 0.891%, respectively. The optimised formulation F11 showing best goodness-fitted model kinetic, followed by Korsmeyer-Peppas equation and zero order kinetic. The SEM and TEM confirmed the spherical and smooth morphology of formulation. FTIR and DSC spectra were given compatibility of compound and XRD diffractograms confirmed the amorphous nature. An ex-vivo study was showed the high permeability coefficient (6.67*1 0 ^-4cm/min, which is twice, compare to pure drug) and there was no damage in nasal mucosa, confirmed by the ciliotoxicity study. In-vivo study was shown significant effects of optimised NLC-DOPA on locomotor activity, force-swimming test and neurochemical assessment using rotenone induced Parkinson's model on Albino Wistar rats.

Conclusion: NLC-DOPA was prepared and optimised successfully with increased bioavailability of drug from the NLC into brain with reduce toxicity in effective treatment of Parkinson's disease.

Propolis has beneficial health properties attributed to of phenolic compounds. However, its application is limited. Thus, encapsulation protects the bioactive compounds of propolis from degradation, allowing their release under controlled and specific conditions and increasing their solubility. In addition to protecting flavonoids, encapsulation also minimises the undesirable characteristics of propolis, such as strong odour. We brought attention to the high antioxidant and antimicrobial activities of encapsulated propolis, and its maintained biological activity enables more uses in different areas. Encapsulated propolis can be applied in food products as an ingredient. This review describes recent advances in improving the bioactivity of propolis extracts by using encapsulation techniques, and biopolymer research strategies, focusing on applications in food products. Encapsulated propolis has a promising market perspective due to the industrial and scientific-technological advancement, the increase in the amount of research, the improvement of propolis extraction techniques, and the need of consumers for innovative products.

The aim of this study was to enhance the dissolution rate and oral bioavailability of herpetetrone (HPT) by preparing nanosuspensions (NSs) and evaluate the changes in its anti-hepatic fibrosis effect. Herpetetrone nanosuspension (HPT-NS) was prepared using the ultrasound-precipitation technique, and characterised on the basis of mean diameter, zeta potential (ZP), encapsulation efficiency percent (EE%), scanning electron microscopy (SEM), and X-ray powder diffraction (XRPD). In addition, the pharmacokinetics and anti-hepatic fibrosis activity were evaluated. HPT-NS prepared with the optimised formulation was found to be spherical with mean diameter of 177.48 ± 6.13 nm, polydispersity index (PDI) of 0.108 ± 0.002 and ZP of -17.28 ± 2.02 mV. The EE (m/m, %) was 83.25 ± 0.27. XRPD analyses confirmed that the amorphous state of HPT in HPT-NS remained unchanged. The dissolution rate of HPT-NS was significantly higher than that of HPT coarse suspensions (HPT-CSs). Following oral administration, C_max and AUC_0-t of HPT-NS showed a significant increase (p < 0.05). In vitro, HPT inhibited the proliferation of HSC-T6 cells and induced apoptosis by up-regulating the expression of Bax proteins and down-regulating the expression of Bcl-2 and TGF-β1 proteins. Compared with HPT-CS, HPT-NS exhibited a more pronounced anti-fibrotic effect. HPT-NS, as a new drug formulation designed to improve the solubility and bioavailability of the drug, shows promising potential in enhancing the anti-liver fibrosis effect.

To improve the stability of fucoxanthin, fucoxanthin liposomes (L) were prepared by the thin-film ultrasound method, and fucoxanthin liposomes were modified with sodium alginate and chitosan by an electrostatic deposition method. The release characteristics of fucoxanthin in different types of liposomes with in vitro gastrointestinal simulation were studied. Under the optimum conditions, the results showed that the encapsulation efficiency of prepared liposomes could reach 88.56 ± 1.40% (m/m), with an average particle size of 295.27 ± 7.28 nm, a Zeta potential of -21.53 ± 2.00 mV, a polydispersity index (PDI) of 0.323 ± 0.007 and a loading capacity of 33.3 ± 0.03% (m/m). Compared with L and chitosan modified fucoxanthin liposomes (CH), sodium alginate and chitosan modified fucoxanthin liposomes (SA-CH) exhibited higher storage stability, in vitro bioaccessibility and antioxidant activity after gastrointestinal digestion. Sodium alginate and chitosan co-modified liposomes can be developed as formulations for encapsulation and delivery of functional ingredients, providing a theoretical basis for developing new fucoxanthin series products.

This study aims to evaluate the radioprotective effects of liposomes encapsulating curcumin (Lip-CUR), silibinin (Lip-SIL), α-tocopherol (Lip-TOC), quercetin (Lip-QUE) and resveratrol (Lip-RES) in alleviating the adverse effects of ionising irradiation on human lymphoctyes and skin cells in radiotherapy. Liposomes encapsulating the above natural radioprotectants (Lip-NRPs) were prepared by the film hydration method combined with sonication. Their radioprotective effects for the cells against X-irradiation was evaluated using trypan-blue assay and γ-H2AX assay. All prepared Lip-NRPs had a mean diameter less than 240 nm, polydispersity index less than 0.32, and zeta potential more than -23 mV. Among them, the radioprotective effect of Lip-RES was lowest, while that of Lip-QUE was highest. Lip-SIL also exhibited a high radioprotective effect despite its low DPPH-radical scavenging activity (12.9%). The radioprotective effects of Lip-NRPs do not solely depend on the free radical scavenging activity of NRPs but also on their ability to activate cellular mechanisms.

Aim: Present study focuses on the development of P80 coated PLGA Nanoparticles loaded with drugs, paroxetine (P80-Par-PLGA-NPs) and clonidine (P80-CLD-PLGA-NPs) for in-vitro evaluation of Cellular Uptake & Cytotoxicity on Neuro-2a cells.

Method: P80-Par-PLGA-NPs and P80-CLD-PLGA-NPs were developed and characterised for zeta size, potential, PDI, EE%, DL%, TEM, SEM, FTIR, DSC, in-vitro release, cytotoxicity, histopathological and cell uptake studies using rhodamine loaded P80-NPs.

Result: Mean particle diameter of P80-Par-PLGA-NPs and P80-CLD-PLGA-NPs was 204; 182.7 nm, ZP of -21.8; -18.72 mV and 0.275; 0.341 PDI, respectively. TEM and SEM images revealed homogenous surface morphology. In-vitro drug release showed sustained and complete release in 72 h. Cell viability (>90%) at C_max and no cytotoxicity in histopathology was observed. Significant higher uptake (96.9%) of P80-modified-NPS was observed as compared to unmodified-NPs (81%) (p < 0.05).

Conclusion: The finding clearly indicated a higher cell uptake of drugs via surface modified P80-coated PLGA-NPs as compared to unmodified particles.