Preparation and evaluation of an oral mucoadhesive gel containing nystatin-loaded alginate microparticles

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
S. Mohammadi Samani ◽  
S. Karimaddini ◽  
Z. Sobhani ◽  
F. Ahmadi
Keyword(s):  
Calcium Chloride ◽  
Encapsulation Efficiency ◽  
Bitter Taste ◽  
Drug Loading ◽  
Dosage Forms ◽  
Release Profile ◽  
Burst Release ◽  
Carbopol Gel ◽  
Alginate Concentration ◽  
Preparation And Evaluation

Abstract Nystatin is an antifungal agent used for prophylaxis and treatment of candidiasis, especially oral mycosis. Efficacy of nystatin conventional dosage forms is limited by the short residence time and bitter taste of the drug. This research aims at designing an optimized formulation of oral mucoadhesive gel of nystatin-loaded alginate microparticles, which can be retained in the mouth. Sodium alginate solution containing nystatin was added to the solution of calcium chloride under stirring. Microparticles containing nystatin were incorporated into the Carbopol gel. Size, loading, and release profile and mucoadhesion were investigated. The most suitable microparticles with particle size of < 250 μm were prepared with alginate concentration of 1%(w/v), calcium chloride of 1%(w/v), drug:polymer concentration 1%, and ratio of alginate solution:calcium chloride of 1:10. This formulation showed 49.1% drug loading and 98.2% encapsulation efficiency. Carbopol 934 gel provided optimal mucoadhesive properties. Release profile proved a burst release, which can be attributed to the surface associated drug, followed by a slower sustained release phase for all microparticles. The developed system with ability to adhere to the oral mucosa has great appeal for treatment of localized infections and can mask bitter taste of the drug and be retained in the mouth for long periods.

scholarly journals Sodium Alginate Nanoparticles of Isoniazid: Preparation and Evaluation

2019 ◽  
Vol 11 (06) ◽  
Author(s):  
Sumit Kumar ◽  
Dinesh Chandra Bhatt
Keyword(s):  
Particle Size ◽  
Sodium Alginate ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Average Particle Size ◽  
Average Particle ◽  
In Vitro Drug Release ◽  
Ionotropic Gelation ◽  
Preparation And Evaluation

Fabrication and evaluation of the Isoniazid loaded sodium alginate nanoparticles (NPs) was main objective of current investigation. These NPs were engineered using ionotropic gelation technique. The NPs fabricated, were evaluated for average particle size, encapsulation efficiency, drug loading, and FTIR spectroscopy along with in vitro drug release. The particle size, drug loading and encapsulation efficiency of fabricated nanoparticles were ranging from 230.7 to 532.1 nm, 5.88% to 11.37% and 30.29% to 59.70% respectively. Amongst all batches studied formulation F-8 showed the best sustained release of drug at the end of 24 hours.

scholarly journals Inulin-Grafted Stearate (In-g-St) as the Effective Self-Assembling Polymeric Micelle: Synthesis and Evaluation for the Delivery of Betamethasone

2020 ◽  
Vol 2020 ◽  
pp. 1-8
Author(s):  
Gholamabbas Chehardoli ◽  
Parham Norouzian ◽  
Farzin Firozian
Keyword(s):  
Zeta Potential ◽  
Sustained Release ◽  
Targeted Delivery ◽  
Encapsulation Efficiency ◽  
Polymeric Micelles ◽  
Drug Loading ◽  
Polymeric Micelle ◽  
Water Soluble ◽  
Burst Release ◽  
Potential Measurement

Background. Betamethasone as a corticosteroid drug is commonly used for the treatment of rheumatoid arthritis. Unfortunately, betamethasone is a low water-soluble drug and its efficacy is low. So an attractive strategy is the targeted delivery of betamethasone to the damaged joint using polymeric micelle-based carriers. Methods. Inulin-grafted stearate (In-g-St) was synthesized via the reaction of stearoyl chloride and inulin, then characterized by FT-IR and H-NMR. In-g-St forms micelles in the presence of betamethasone. The prepared polymeric micelles were characterized for size, zeta potential, drug loading, particles’ morphology, critical micelle concentration (CMC), and encapsulation efficiency. So sustained release polymeric micelles of betamethasone were developed by employing In-g-St. Results. The measurement of particle size showed a mean diameter of 60 and 130 nm for 10% and 20% drug-loaded micelles, respectively, and SEM showed that the particle’s morphologies are spherical. Zeta potential measurement for the drug-containing micelles showed a value of -11.8 mV. Drug loading efficiency and the encapsulation efficiency were 6.36% and 63.6%, as well as 18.97% and 94.88% for 10% and 20%, respectively. 20% drug-loaded polymer showed a small burst release of betamethasone at the first 3 h which was followed by sustained release in the next 24 h. Furthermore, the formula with 10% exhibited good sustained release properties except for the minor initial burst release. Conclusion. Data from the zeta potential, CMC, drug loading capacity, and in vitro drug release studies indicated that In-g-St polymeric micelles can be suitable candidates for the efficient delivery of hydrophobic drugs like betamethasone.

In vitro drug release and antibacterial activity evaluation of silk fibroin coated vancomycin hydrochloride loaded poly (lactic-co-glycolic acid) (PLGA) sustained release microspheres

2022 ◽  
pp. 088532822110640
Author(s):  
Shengtang Li ◽  
Xuewen Shi ◽  
Bo Xu ◽  
Jian Wang ◽  
Peng Li ◽  
...  
Keyword(s):  
Drug Release ◽  
Encapsulation Efficiency ◽  
Glycolic Acid ◽  
Drug Loading ◽  
Burst Release ◽  
Plga Microspheres ◽  
In Vitro Drug Release ◽  
Initial Burst ◽  
Initial Burst Release

Currently, the treatment of osteomyelitis poses a great challenge to clinical orthopedics. The use of biodegradable materials combined with antibiotics provides a completely new option for the treatment of osteomyelitis. In this study, vancomycin hydrochloride (VANCO) loaded poly (lactic-co-glycolic acid) (PLGA) microspheres were prepared by a double emulsion solvent evaporation method, and the in vitro drug release behaviors of the drug loaded microspheres were explored after coating with different concentrations of silk fibroin (SF). Drug loading, encapsulation efficiency, Scanning electron microscopy, particle size analysis, Fourier transform infrared spectroscopy, hydrophilicity, in vitro drug release, and in vitro antibacterial activity were evaluated. The results showed that the drug loading of vancomycin loaded PLGA microspheres was (24.11 ±1.72)%, and the encapsulation efficiency was (48.21 ±3.44)%. The in vitro drug release indicated that the drug loaded microspheres showed an obvious initial burst release, and the drug loaded microspheres coated with SF could alleviate the initial burst release in varying degrees. It also can reduce the amount of cumulative drug release, and the effect of microspheres coated with 0.1% concentration of SF is the best. The time of in vitro drug release in different groups of drug loaded microspheres can be up to 28 days. The microspheres coated with (0.1%SF) or without (0%SF) SF showed a cumulative release of (82.50±3.51)% and (67.70±3.81)%,respectively. Therefore, the surface coating with SF of vancomycin loaded microspheres can alleviate the initial burst release, reduce the cumulative drug release, potentially prolong the drug action time, and improve the anti-infection effect.

Alginate–Chitosan Nanocapsules for Controlled Release of Low Molecular Drugs Tegafur and DHAD

2013 ◽  
Vol 647 ◽  
pp. 264-268 ◽  
Author(s):  
Yuan Gang Liu ◽  
Hong Hao Mao ◽  
Shi Bin Wang ◽  
Qing Qing Sun
Keyword(s):  
Controlled Release ◽  
Release Rate ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Burst Release ◽  
Two Stage ◽  
Cumulative Release ◽  
Stage Process

Alginate–chitosan nanocapsules (Alg-CS NCs) were prepared by a two-stage process. The NCs were loaded with two low molecular drugs-tegafur and Mitoxantrone Hydrochloride(DHAD). Results revealed that these two drugs exhibited different drug loading and release characteristics. The drug loading and encapsulation efficiency of tegafur (<1%) were both lower than those of DHAD with the drug loading at about 20%~60% and encapsulation efficiency over 90%. However, tegafur showed a visible burst release phenomenon and the cumulative release rate of tegafur was much higher than that of DHAD.

scholarly journals Fabrication of Bio-Nanocomposite Based on HNT-Methionine for Controlled Release of Phenytoin

Polymers ◽  
2021 ◽  
Vol 13 (15) ◽  
pp. 2576
Author(s):  
Majid Abdouss ◽  
Nastaran Radgoudarzi ◽  
Alireza Mohebali ◽  
Elaheh Kowsari ◽  
Mojtaba Koosha ◽  
...  
Keyword(s):  
Controlled Release ◽  
Zeta Potential ◽  
Encapsulation Efficiency ◽  
Release Profile ◽  
Burst Release ◽  
Loading Efficiency ◽  
Phenytoin Sodium ◽  
Good Potential ◽  
Ft Ir

In this study, a novel promising approach for the fabrication of Halloysite nanotube (HNT) nanocomposites, based on the amino acid named Methionine (Met), was investigated. For this purpose, Met layered on the outer silane functionalized surface of HNT for controlled release of Phenytoin sodium (PHT). The resulting nanocomposite (MNT-g-Met) was characterized by FTIR, XRD, Zeta potential, TGA, TEM and FE-SEM. The FT-IR results showed APTES and Met peaks, which proved the modification of the HNTs. The zeta-potential results showed the interaction between APTES (+53.30) and Met (+38.80) on the HNTs (−30.92). The FE-SEM micrographs have displayed the grafting of Met on the modified HNTs due to the nanotube conversion to a rough and indistinguishable form. The amount of encapsulation efficiency (EE) and loading efficiency (LE) of MNT-g-Met was 74.48% and 37.24%, while pure HNT was 57.5%, and 28.75%, respectively. In-vitro studies showed that HNT had a burst release (70% in 6 h) in phosphate buffer while MNT-g-Met has more controlled release profile (30.05 in 6 h) and it was found to be fitted with the Korsmeyer-Peppas model. Due to the loading efficiency and controlled release profile, the nanocomposite promote a good potential for drug delivery of PHT.

scholarly journals Preparation of Silymarin–quercetin Loaded Nanoparticles by Spontaneous Emulsification Solvent Diffusion Method Using D-alpha-tocopheryl Poly (Ethylene Glycol) 1000 Succinate

2021 ◽  
pp. 84-94
Author(s):  
S. Senthila ◽  
P. Manoj Kumar ◽  
P. Venkatesan
Keyword(s):  
Electron Microscopy ◽  
Drug Release ◽  
Ethylene Glycol ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Release Profile ◽  
Poly Ethylene Glycol ◽  
Drug Release Profile ◽  
Spontaneous Emulsification ◽  
Poly Ethylene

Silymarin, a flavonolignan, derived from Silybum marianum, family Asteraceae has long been used as a hepatoprotective remedy. Silymarin has cytoprotective activities due to its antioxidant property and free radical scavenging activity. The pharmacokinetic studies of past three decades revealed that silymarin has poor absorption, rapid metabolism especially by Phase II metabolism and ultimately poor oral bioavailability. Quercetin, a flavonoid present in edible vegetables and fruits, It is a potent antioxidant and shows a wide range of biological functions. Quercetin improves blood levels and efficacy of number of drugs since it is P-Glycoprotein inhibitor and also inhibits drug metabolizing enzymes. Both silymarin and quercetin were, poorly soluble in the water shows low bioavailability. The advanced type of formulation like polymeric nanoparticles (PNPs) can be successfully utilised for bioavailability enhancement and targeting the Silymarin-quercetin to hepatocytes. A controlled release PNPs of silymarin-quercetin were prepared by spontaneous emulsification solvent diffusion (SESD) method using Poly Lactic-co-Glycolic Acid (PLGA) as biodegradable polymer, D-alpha-tocopheryl poly (ethylene glycol) 1000 succinate (TPGS) used as a solubilizer, as an emulsifier. TPGS as an emulsifier and further as a matrix material blended with PLGA was used to enhance the encapsulation efficiency and improve the drug release profile of nanoparticles. Different formulations with various drug: polymer ratios and volume and concentration of surfactant, centrifugation time were evaluated. The effect of formulation parameters such as drug/polymer ratio, volume and surfactant content were evaluated. The surface morphology and size of the nanoparticles were studied by scanning electron microscopy (SEM) Transmission electron microscopy (TEM). Drug encapsulation efficiency and in vitro drug release profiles of nanoparticles were determined using UV spectrophotometry. The nanoparticles prepared with combination of both the drugs in this study were spherical with size range of 100–200 nm. It was shown that TPGS was a good emulsifier for producing nanoparticles of hydrophobic drugs and improving the encapsulation efficiency and drug loading and drug release profile of nanoparticles. Although the amount of the TPGS used had a significant effect on the nanoparticle size and morphology, the drug loading and release profile of nanoparticles

scholarly journals Tailor-Made Pentablock Copolymer Based Formulation for Sustained Ocular Delivery of Protein Therapeutics

2014 ◽  
Vol 2014 ◽  
pp. 1-15 ◽  
Author(s):  
Sulabh P. Patel ◽  
Ravi Vaishya ◽  
Gyan Prakash Mishra ◽  
Viral Tamboli ◽  
Dhananjay Pal ◽  
...  
Keyword(s):  
Drug Loading ◽  
Entrapment Efficiency ◽  
Polyglycolic Acid ◽  
Cd Spectroscopy ◽  
Protein Therapeutics ◽  
Release Profile ◽  
Hydrodynamic Diameter ◽  
Burst Release ◽  
Thermosensitive Gel

The objective of this research article is to report the synthesis and evaluation of novel pentablock copolymers for controlled delivery of macromolecules in the treatment of posterior segment diseases. Novel biodegradable PB copolymers were synthesized by sequential ring-opening polymerization. Various ratios and molecular weights of each block (polyglycolic acid, polyethylene glycol, polylactic acid, and polycaprolactone) were selected for synthesis and to optimize release profile of FITC-BSA, IgG, and bevacizumab from nanoparticles (NPs) and thermosensitive gel. NPs were characterized for particle size, polydispersity, entrapment efficiency, and drug loading. In vitro release study of proteins from NPs alone and composite formulation (NPs suspended in thermosensitive gel) was performed. Composite formulations demonstrated no or negligible burst release with continuous near zero-order release in contrast to NPs alone. Hydrodynamic diameter of protein therapeutics and hydrophobicity of PB copolymer exhibited significant effect on entrapment efficiency and in vitro release profile. CD spectroscopy confirmed retention of structural conformation of released protein. Biological activity of released bevacizumab was confirmed by in vitro cell proliferation and cell migration assays. It can be concluded that novel PB polymers can serve a platform for sustained delivery of therapeutic proteins.

scholarly journals Influence of Sodium Alginate on Hypoglycemic Activity of Metformin Hydrochloride in the Microspheres Obtained by the Spray Drying

2016 ◽  
Vol 2016 ◽  
pp. 1-12 ◽  
Author(s):  
Marta Szekalska ◽  
Magdalena Wróblewska ◽  
Katarzyna Sosnowska ◽  
Katarzyna Winnicka
Keyword(s):  
Sodium Alginate ◽  
Spray Drying ◽  
Drug Loading ◽  
Release Profile ◽  
Hypoglycemic Activity ◽  
Metformin Hydrochloride ◽  
Drying Method ◽  
Alginate Concentration ◽  
Polymer Ratio

Alginate microspheres with metformin hydrochloride were prepared by the spray drying method in order to improve residence time of drug in the stomach. Nine formulations (F1–F9) with various drug : polymer ratio (1 : 2, 1 : 1, and 2 : 1) and different sodium alginate concentration (1%, 2%, and 3%) were evaluated for size, morphology, drug loading, Zeta potential, and swelling degree.In vitrodrug release, mathematical release profile, and physical state of microspheres were also evaluated. Optimal formulation characterized by the highest drug loading was formulation F6 (drug : polymer ratio 2 : 1 and 2% alginate solution). Based on glucose uptake inSaccharomyces cerevisiaecells andα-amylase inhibition tests, it could be concluded that alginate microspheres enhance hypoglycemic activity of metformin hydrochloride evaluatedin vitro. Designed microspheres are promising as alternative, multicompartment dosage form for metformin hydrochloride delivery.

scholarly journals Biodegradable Nanoparticles-Loaded PLGA Microcapsule for the Enhanced Encapsulation Efficiency and Controlled Release of Hydrophilic Drug

2021 ◽  
Vol 22 (6) ◽  
pp. 2792
Author(s):  
Suji Ryu ◽  
Seungyeop Park ◽  
Ha Yeon Lee ◽  
Hyungjun Lee ◽  
Cheong-Weon Cho ◽  
...  
Keyword(s):  
Controlled Release ◽  
Side Effects ◽  
Sustained Release ◽  
Encapsulation Efficiency ◽  
Release Profile ◽  
Burst Release ◽  
Initial Burst ◽  
Initial Burst Release ◽  
Chitosan Coating ◽  
Hydrophilic Drug

Recently, nano- and micro-particulate systems have been widely utilized to deliver pharmaceutical compounds to achieve enhanced therapeutic effects and reduced side effects. Poly (DL-lactide-co-glycolide) (PLGA), as one of the biodegradable polyesters, has been widely used to fabricate particulate systems because of advantages including controlled and sustained release, biodegradability, and biocompatibility. However, PLGA is known for low encapsulation efficiency (%) and insufficient controlled release of water-soluble drugs. It would result in fluctuation in the plasma levels and unexpected side effects of drugs. Therefore, the purpose of this work was to develop microcapsules loaded with alginate-coated chitosan that can increase the encapsulation efficiency of the hydrophilic drug while exhibiting a controlled and sustained release profile with reduced initial burst release. The encapsulation of nanoparticles in PLGA microcapsules was done by the emulsion solvent evaporation method. The encapsulation of nanoparticles in PLGA microcapsules was confirmed by scanning electron microscopy and confocal microscopy. The release profile of hydrophilic drugs can further be altered by the chitosan coating. The chitosan coating onto alginate exhibited a less initial burst release and sustained release of the hydrophilic drug. In addition, the encapsulation of alginate nanoparticles and alginate nanoparticles coated with chitosan in PLGA microcapsules was shown to enhance the encapsulation efficiency of a hydrophilic drug. Based on the results, this delivery system could be a promising platform for the high encapsulation efficiency and sustained release with reduced initial burst release of the hydrophilic drug.

Extrusion-Based 3D Printing for Pharmaceuticals: Contemporary Research and Applications

2019 ◽  
Vol 24 (42) ◽  
pp. 4991-5008 ◽  
Author(s):  
Mohammed S. Algahtani ◽  
Abdul Aleem Mohammed ◽  
Javed Ahmad
Keyword(s):  
Cosmetic Surgery ◽  
Fused Deposition Modeling ◽  
Personalised Medicine ◽  
Organ Transplant ◽  
Three Dimensional ◽  
Dosage Forms ◽  
Release Profile ◽  
Small Scale ◽  
Drug Release Profile ◽  
Fused Deposition

Three-dimensional printing (3DP) has a significant impact on organ transplant, cosmetic surgery, surgical planning, prosthetics and other medical fields. Recently, 3 DP attracted the attention as a promising method for the production of small-scale drug production. The knowledge expansion about the population differences in metabolism and genetics grows the need for personalised medicine substantially. In personalised medicine, the patient receives a tailored dose and the release profile is based on his pharmacokinetics data. 3 DP is expected to be one of the leading solutions for the personalisation of the drug dispensing. This technology can fabricate a drug-device with complicated geometries and fillings to obtain the needed drug release profile. The extrusionbased 3 DP is the most explored method for investigating the feasibility of the technology to produce a novel dosage form with properties that are difficult to achieve using the conventional industrial methods. Extrusionbased 3 DP is divided into two techniques, the semi-solid extrusion (SSE) and the fused deposition modeling (FDM). This review aims to explain the extrusion principles behind the two techniques and discuss their capabilities to fabricate novel dosage forms. The advantages and limitations observed through the application of SSE and FDM for fabrication of drug dosage forms were discussed in this review. Further exploration and development are required to implement this technology in the healthcare frontline for more effective and personalised treatment.

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