Preparation and evaluation of a stable and sustained release of lansoprazole-loaded poly(d,l-lactide-co-glycolide) polymeric nanoparticles

Abstract The aim of the study was to prepare lansoprazole (LNS)-loaded poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles in order to improve the physicochemical stability associated with LNS. We synthesized LNS-loaded PLGA nanoparticles in the presence of magnesium oxide as alkalizer to improve the release of LNS and stability against photodegradation. The LNS-encapsulated PLGA nanoparticles were developed by the nanoprecipitation/solvent evaporation method, resulting in a particle size of 246.7 ± 3.4 nm, polydispersity index (PDI) of 0.126, percent drug entrapment (PDE) of 82.85 ± 4.5%, percent drug loading (PDL) of 3.54 ± 0.34%, and pH of 8.10 ± 0.56. The developed nanoparticles were further evaluated for in vitro release and resistance to photodegradation by NMR spectroscopy and LC-MS. The sustained release of the drug was confirmed after the encapsulation of LNS in the PLGA matrix. The protection of LNS in the PLGA matrix against photodegradation was confirmed by NMR and LC-MS studies. The LC-MS of UV-exposed samples of pure LNS and LNS-loaded PLGA nanoparticles at 254 nm showed the same (M + 1) peak at 370 m/e, and the base peak at 369 m/e accounted for the unchanged structure of LNS inside PLGA nanoparticles. Overall, it was proved that PLGA nanoparticles in the presence of magnesium oxide are an efficient carrier to deliver and protect LNS from physicochemical instability.

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Preparation and Release Profiles in Vitro/Vivo of Galantamine Pamoate Loaded Poly (Lactideco-Glycolide) (PLGA) Microspheres

Frontiers in Pharmacology ◽

10.3389/fphar.2020.619327 ◽

2021 ◽

Vol 11 ◽

Author(s):

Liping Du ◽

Shankui Liu ◽

Guizhou Hao ◽

Li Zhang ◽

Miaomiao Zhou ◽

...

Keyword(s):

Drug Release ◽

Sustained Release ◽

Drug Loading ◽

Entrapment Efficiency ◽

Solvent Evaporation Method ◽

Sustained Drug Release ◽

Water Emulsion ◽

Oil Water

Patient’s poor compliance and the high risk of toxic effects limit the clinical use of galantamine hydrobromide. To overcome these drawbacks, the sustained-release galantamine pamoate microspheres (GLT-PM-MS) were successfully developed using an oil/water emulsion solvent evaporation method in this study. Physicochemical properties of GLT-PM-MS were carefully characterized, and the in vitro and in vivo drug release behaviors were well studied. Results showed that the morphology of optimized microspheres were spherical with smooth surfaces and core-shell interior structure. Mean particle size, drug loading and entrapment efficiency were 75.23 ± 1.79 μm, 28.01 ± 0.81% and 87.12 ± 2.71%, respectively. The developed GLT-PM-MS were found to have a sustained release for about 24 days in vitro and the plasma drug concentration remained stable for 17 days in rats. These results indicated that GLT-PM-MS could achieve the sustained drug release purpose and be used in clinical trial.

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Encapsulation of Andrographolide in poly(lactide-co-glycolide) Nanoparticles: Formulation Optimization and in vitro Efficacy Studies

Frontiers in Bioengineering and Biotechnology ◽

10.3389/fbioe.2021.639409 ◽

2021 ◽

Vol 9 ◽

Author(s):

Bukola A. Oseni ◽

Chukwuemeka P. Azubuike ◽

Omotunde O. Okubanjo ◽

Cecilia I. Igwilo ◽

Jayanth Panyam

Keyword(s):

Sustained Release ◽

Organic Solvent ◽

Drug Loading ◽

Metastatic Breast ◽

Plga Nanoparticles ◽

Polymer Composition ◽

Molecular Weight Polymer ◽

Anticancer Efficacy ◽

Efficacy Studies

Andrographolide is a potential chemopreventive and chemotherapeutic agent that suffers from poor aqueous solubility. Encapsulation in poly(lactide-co-glycolide) (PLGA) nanoparticles can overcome solubility issues and enable sustained release of the drug, resulting in improved therapeutic efficacy. In this study, andrographolide was encapsulated in PLGA nanoparticles via emulsion solvent evaporation technique. Effect of various formulation parameters including polymer composition, polymer molecular weight, polymer to drug ratio, surfactant concentration and the organic solvent used on nanoparticle properties were investigated. A selected formulation was used to determine the effect of encapsulation in nanoparticles on andrographolide’s in vitro anticancer efficacy. Nanoparticles formulated using a polymer with 85:15 lactide to glycolide ratio and ethyl acetate as the organic solvent were found to be optimal based on average hydrodynamic particle size (135 ± 4 nm) and drug loading (2.6 ± 0.6%w/w). This formulation demonstrated sustained release of andrographolide over 48 h and demonstrated significantly greater in vitro anticancer efficacy compared to free drug in a metastatic breast cancer cell line. These results suggest that additional, more in-depth efficacy studies are warranted for the nanoparticle formulation of andrographolide.

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Preparation and in vitro Evaluation of Bioadhesive Microparticulate System

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2008.1.3.9 ◽

1970 ◽

Vol 1 (3) ◽

pp. 257-266

Author(s):

Nagda C. D. ◽

Chotai N. P. ◽

Patel S. B. ◽

Soni T. J ◽

Patel U. L

Keyword(s):

Drug Loading ◽

In Vitro Release ◽

Phenyl Acetic Acid ◽

Solvent Evaporation Method ◽

Elimination Half ◽

Release Studies ◽

Differential Scanning Colorimetry ◽

Polymer Interactions ◽

Vitro Release

Aceclofenac (ACE) is NSAIDs of a phenyl acetic acid class. It is indicated in arthritis and osteoarthritis, rheumatoid arthritis, ankylosing spondylitis. It has short elimination half life of 4 hours. The objective of the study is to design, characterize and evaluate bioadhesive microspheres of ACE employing carbopol (CP) as bioadhesive polymer. Bioadhesive microspheres of ACE were prepared by solvent evaporation method. The prepared microspheres were free flowing and spherical in shape and characterized for drug loading, mucoadhesion test, infrared spectroscopy (IR), differential scanning colorimetry (DSC) and scanning electron microscopy (SEM). The in-vitro release studies were performed using pH 6.8 phosphate buffer. The drug loaded microspheres in a ratio of 1:5 showed 47% of drug entrapment; percentage mucoadhesion was 81% and 89% release in 10 h. The infrared spectra and DSC showed stable character of aceclofenac in the drug loaded microspheres and revealed the absence of drug-polymer interactions. SEM studies showed that the microspheres are spherical and porous in nature. The in vitro release profiles from microspheres of different polymer-drug ratios followed Higuchi model.

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Preparation, evaluation, and in vitro release of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules

Technology and Health Care ◽

10.3233/thc-202529 ◽

2020 ◽

pp. 1-9

Author(s):

Yunhong Wang ◽

Rong Hu ◽

Yanlei Guo ◽

Weihan Qin ◽

Xiaomei Zhang ◽

...

Keyword(s):

Drug Release ◽

Sustained Release ◽

Release Rate ◽

Orthogonal Design ◽

Drug Loading ◽

In Vitro Release ◽

Core Material ◽

Evaluation Indexes ◽

Vitro Release

OBJECTIVE: In this study we explore the method to prepare tanshinone self-microemulsifying sustained-release microcapsules using tanshinone self-microemulsion as the core material, and chitosan and alginate as capsule materials. METHODS: The optimal preparation technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules was determined by using the orthogonal design experiment and single-factor analysis. The drug loading and entrapment rate were used as evaluation indexes to assess the quality of the drug, and the in vitro release rate was used to evaluate the drug release performance. RESULTS: The best technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules is as follows: the concentration of alginate is 1.5%, the ratio of tanshinone self-microemulsion volume to alginate volume to chitosan mass is 1:1:0.5 (ml: ml: g), and the best concentration of calcium chloride is 2.0%. To prepare the microcapsules using this technology, the drug loading will be 0.046%, the entrapment rate will be 80.23%, and the 24-hour in vitro cumulative release rate will be 97.4%. CONCLUSION: The release of the microcapsules conforms to the Higuchi equation and the first-order drug release model and has a good sustained-release performance.

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Development of In Situ Self-Assembly Nanoparticles to Encapsulate Lopinavir and Ritonavir for Long-Acting Subcutaneous Injection

Pharmaceutics ◽

10.3390/pharmaceutics13060904 ◽

2021 ◽

Vol 13 (6) ◽

pp. 904

Author(s):

Irin Tanaudommongkon ◽

Asama Tanaudommongkon ◽

Xiaowei Dong

Keyword(s):

Sustained Release ◽

Trough Concentration ◽

Self Assembly ◽

Subcutaneous Injection ◽

Drug Loading ◽

Entrapment Efficiency ◽

Long Acting

Most antiretroviral medications for human immunodeficiency virus treatment and prevention require high levels of patient adherence, such that medications need to be administered daily without missing doses. Here, a long-acting subcutaneous injection of lopinavir (LPV) in combination with ritonavir (RTV) using in situ self-assembly nanoparticles (ISNPs) was developed to potentially overcome adherence barriers. The ISNP approach can improve the pharmacokinetic profiles of the drugs. The ISNPs were characterized in terms of particle size, drug entrapment efficiency, drug loading, in vitro release study, and in vivo pharmacokinetic study. LPV/RTV ISNPs were 167.8 nm in size, with a polydispersity index of less than 0.35. The entrapment efficiency was over 98% for both LPV and RTV, with drug loadings of 25% LPV and 6.3% RTV. A slow release rate of LPV was observed at about 20% on day 5, followed by a sustained release beyond 14 days. RTV released faster than LPV in the first 5 days and slower than LPV thereafter. LPV trough concentration remained above 160 ng/mL and RTV trough concentration was above 50 ng/mL after 6 days with one subcutaneous injection. Overall, the ISNP-based LPV/RTV injection showed sustained release profiles in both in vitro and in vivo studies.

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Preparation and evaluation of sustained-release azithromycin tablets in vitro and in vivo

Asian Journal of Pharmaceutical Sciences ◽

10.1016/j.ajps.2014.03.003 ◽

2014 ◽

Vol 9 (3) ◽

pp. 155-161 ◽

Cited By ~ 4

Author(s):

Le Sun ◽

Weixiang Zhang ◽

Xiaohong Liu ◽

Jin Sun

Keyword(s):

Sustained Release ◽

Preparation And Evaluation

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Photodynamic Treatment of Colorectal Cancer Using Chlorin e6-Loaded Poly(lactide-co-glycolide)- Based Nanoparticles

Journal of Biomedical Nanotechnology ◽

10.1166/jbn.2021.3170 ◽

2021 ◽

Vol 17 (10) ◽

pp. 1939-1950

Author(s):

Beibei Lin ◽

Xuegu Xu ◽

Xiaobi Zhang ◽

Yinfei Yu ◽

Xiaoling Wang

Keyword(s):

Colorectal Cancer ◽

Drug Loading ◽

Average Diameter ◽

Plga Nanoparticles ◽

Chlorin E6 ◽

Photodynamic Treatment ◽

Hct 116 ◽

Hct 116 Cells ◽

The Stability

We prepared poly(lactide-co-glycolide) (PLGA) encapsulated with chlorin e6 (Ce6) in an effort to increase the stability and efficiency of photosensitizers for photodynamic therapy (PDT). We determined that Ce6-loaded PLGA nanoparticles (PLGA-Ce6 NPs) had drug-loading efficiency of 5%. The efficiency of encapsulation was 82%, the zeta potential was- 25 mV, and the average diameter was 130 nm. The encapsulation of Ce6 in PLGA nanoparticles showed excellent stability. The nanoparticles exhibited sustained Ce6 release profiles with 50% released at the end of 3 days, whereas free Ce6 showed rapid release within 1 day. Ce6 release patterns were controlled by encapsulation into PLGA. The uptake of PLGA-Ce6 NPs was significantly enhanced by endocytosis in the first 8 hours in the HCT-116 cell line. An intracellular reactive oxygen species assay revealed the enhanced uptake of the nanoparticles. An in vitro anti-tumor activity assay showed that the PLGA-Ce6 NPs exhibited enhanced phototoxicity toward HCT-116 cells and a slightly lower IC50 value in HCT-116 cells than Ce6 solution alone. Exposure of HCT-116 cell spheroids to PLGA-Ce6 NPs penetrated more profoundly and had better phototoxicity than pure drugs. These findings suggest that PLGA-Ce6 NPs might serve as PDT for colorectal cancer.

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FORMULATION AND EVALUATION OF MUCOADHESIVE MICROSPHERES OF AN ANTI-MIGRAINE DRUG

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v8i5.1943 ◽

2018 ◽

Vol 8 (5) ◽

pp. 465-474

Author(s):

S PADMA PRIYA ◽

AN Rajalakshmi ◽

P Ilaveni

Keyword(s):

Drug Release ◽

Sustained Release ◽

Sodium Alginate ◽

Release Kinetics ◽

Drug Loading ◽

Research Work ◽

Entrapment Efficiency ◽

Polyvinyl Pyrrolidone ◽

Anti Migraine Drug

Objective: The objective of this research work is to develop and evaluate mucoadhesive microspheres of an anti-migraine drug for sustained release. Materials and Methods: Mucoadhesive microspheres were prepared by emulsification method using Sodium alginate (SA), polyvinyl pyrrolidone (PVP) and Chitosan in the various drug-polymer ratios of 1:1, 1:2 and 1:3. Nine formulations were formulated and evaluated for possible drug polymer interactions, percentage yield, micromeritic properties, particle size, drug content, drug entrapment efficiency, drug loading, swelling index, In-vitro wash off test, in vitro drug release, surface morphology and release kinetics. Results: The results showed that no significant drug polymer interaction in FTIR studies. Among all the formulations SF3 containing sodium alginate showed 77.18% drug release in 6hrs. Conclusion: Amongst the developed mucoadhesive microspheres, SF3 formulation containing sodium alginate exhibited slow and sustained release in a controlled manner and it is a promising formulation for sustained release of Sumatriptan succinate. Keywords: Mucoadhesive microspheres, Sodium alginate, polyvinyl pyrrolidone, Chitosan, sustained release.

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Sodium Alginate Nanoparticles of Isoniazid: Preparation and Evaluation

International Journal of Pharmaceutical Sciences and Drug Research ◽

10.25004/ijpsdr.2019.110616 ◽

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.

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