Gelatin Methacryloyl Hydrogels for the Localized Delivery of Cefazolin

The tuneability of hydrogels renders them promising candidates for local drug delivery to prevent and treat local surgical site infection (SSI) while avoiding the systemic side-effects of intravenous antibiotic injections. Here, we present a newly developed gelatin methacryloyl (GelMA)-based hydrogel drug delivery system (GelMA-DDS) to locally deliver the broad-spectrum antibiotic cefazolin for SSI prophylaxis and treatment. Antibiotic doses from 3 µg to 90 µg were loaded in photocrosslinked GelMA hydrogel discs with 5 to 15% w/v polymer concentration and drug encapsulation efficiencies, mechanical properties, crosslinking and release kinetics, as well as bacterial growth inhibition were assessed. Our results demonstrate that all GelMA groups supported excellent drug encapsulation efficiencies of up to 99%. Mechanical properties of the GelMA-DDS were highly tuneable and unaffected by the loading of small to medium doses of cefazolin. The diffusive and the proteolytic in vitro drug delivery of all investigated cefazolin doses was characterized by a burst release, and the delivered cefazolin amount was directly proportional to the encapsulated dose. Accelerated enzymatic degradation of the GelMA-DDS followed zero-order kinetics and was dependent on both the cefazolin dose and GelMA concentration (3–13 h). Finally, we demonstrate that cefazolin delivered from GelMA induced a dose-dependent antibacterial efficacy against S. aureus, in both a broth and a diffusive assay. The cefazolin-loaded GelMA-DDS presented here provides a highly tuneable and easy-to-use local delivery system for the prophylaxis and treatment of SSI.

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Applicability of Gum Karaya in the Preparation and in Vitro Evaluation of Losartan Potassium as Chronotherapeutic Drug Delivery System

Journal of Scientific Research ◽

10.3329/jsr.v7i1-2.21182 ◽

2015 ◽

Vol 7 (1-2) ◽

pp. 65-74

Author(s):

K. Latha ◽

V. V. Srikanth ◽

S. A. Sunil ◽

N. R. Srinivasa ◽

M. U. Uhumwangho ◽

...

Keyword(s):

Drug Delivery ◽

Tensile Strength ◽

Drug Delivery System ◽

Delivery System ◽

Lag Time ◽

Losartan Potassium ◽

In Vitro Dissolution ◽

Burst Release ◽

Gum Karaya

The objective of this investigation is to study the applicability of gum karaya, the natural gum for the preparation and in vitro evaluation of losartan potassium, as Chronotherapeutic Drug Delivery System (ChDDS). The compression-coated timed-release tablets (CCT) containing losartan potassium in the core tablet were prepared by dry coating technique with different ratios of gum karaya as the outer coat. The parameters investigated were tensile strength, friability, in vitro dissolution studies and drug concentration. The optimized formulation was further characterized by powder XRD and FTIR to investigate interactions and no interactions observed. The tensile strength and friability of all the CCT were between 1.06-1.23 MN/m2 and < 0.3% respectively. All the CCT showed a clear lag time before a burst release of drug. However, the lag time of drug release increased as the amount of gum karaya in the outer layer increased. For instance, the lag time of LGK1, LGK2, LGK3, LGK4, LGK5, LGK6 and LGK7 were 16, 10.5, 5.5, 3, 2, 1.5 and 0.5 hrs respectively. The drug content of all the CCT was >98%. Formulation LGK3 was taken as an optimized formulation which can be exploited to achieve ChDDS of losartan potassium for the treatment of hypertension.

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Thermosensitive Chitosan Hydrogels Containing Polymeric Microspheres for Vaginal Drug Delivery

BioMed Research International ◽

10.1155/2017/3564060 ◽

2017 ◽

Vol 2017 ◽

pp. 1-12 ◽

Cited By ~ 7

Author(s):

Ting-Ting Yang ◽

Yuan-Zheng Cheng ◽

Meng Qin ◽

Yong-Hong Wang ◽

Hong-Li Yu ◽

...

Keyword(s):

Drug Delivery ◽

Sustained Release ◽

Delivery System ◽

Drug Loading ◽

Great Promise ◽

Burst Release ◽

Bletilla Striata ◽

Vaginal Drug Delivery ◽

Thermosensitive Hydrogels

Thermosensitive hydrogels have increasingly received considerable attention for local drug delivery based on many advantages. However, burst release of drugs is becoming a critical challenge when the hydrogels are employed. Microspheres- (MS-) loaded thermosensitive hydrogels were thus fabricated to address this limitation. Employing an orthogonal design, the spray-dried operations of tenofovir (TFV)/Bletilla striata polysaccharide (BSP)/chitosan (CTS) MS were optimized according to the drug loading (DL). The physicochemical properties of the optimal MS (MS F) were characterized. Depending on the gelation temperature and gelating time, the optimal CTS-sodium alginate- (SA-) α,β-glycerophosphate (GP) (CTS-SA-GP) hydrogel was obtained. Observed by scanning electron microscope (SEM), TFV/BSP/CTS MS were successfully encapsulated in CTS-SA-GP. In vitro releasing demonstrated that MS F-CTS-SA-GP retained desirable in vitro sustained-release characteristics as a vaginal delivery system. Bioadhesion measurement showed that MS-CTS-SA-GP exhibited the highest mucoadhesive strength. Collectively, MS-CTS-SA-GP holds great promise for topical applications as a sustained-release vaginal drug delivery system.

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QbD-Based Development and Evaluation of Time-dependent Chronopharmaceutical Drug Delivery System of Amoxicillin Trihydrate for Management of Bacterial Infection

International Journal of Pharmaceutical Sciences and Drug Research ◽

10.25004/ijpsdr.2018.100311 ◽

2018 ◽

Vol 10 (03) ◽

Author(s):

Shyam Narayan Prasad ◽

Ashok Kumar Sahoo ◽

Abhijit V. Gothoskar

Keyword(s):

Drug Delivery ◽

Bacterial Infection ◽

Drug Delivery System ◽

Delivery System ◽

Bacterial Infections ◽

Release Kinetics ◽

Matrix Tablets ◽

Critical Material ◽

Amoxicillin Trihydrate

The present studies discuss about the quality by design (QbD)-based development and evaluation of chronomodulated release drug delivery system of amoxicillin trihydrate for management of bacterial infection. Initially, target product profile was defined and critical quality attributes were earmarked. Risk assessment study was performed for identifying the critical material attributes. Preformulation studies were carried out, and direct compression method was employed for the preparation of bilayer matrix tablets containing a delayed and a sustained release layer for preliminary optimization. Systematic formulation optimization was carried out using central composite design by selecting the concentration of Eudragit-L100 D55 and HPMCK4M. Mathematical modeling was performed and optimized compositions of the polymers were identified from the design space. Moreover, the prepared bilayer tablets were evaluated for various tablet properties including in vitro drug release study, release kinetics evaluation and characterized for FTIR, DSC, XRD, SEM studies, in vitro was-off test, antimicrobial assay and accelerated stability studies. In a nutshell, the present studies indicated the supremacy of designing a chronomodulated release bilayer tablet formulations of amoxicillin trihydrate for effective management of bacterial infections.

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Understanding the burst release phenomenon: toward designing effective nanoparticulate drug-delivery systems

Therapeutic Delivery ◽

10.4155/tde-2020-0099 ◽

2020 ◽

pp. 00-00

Author(s):

Sourav Bhattacharjee

Keyword(s):

Drug Delivery ◽

Sustained Release ◽

Mathematical Models ◽

Drug Delivery Systems ◽

Release Kinetics ◽

Burst Release ◽

Future Directions ◽

Short Period

Burst release of encapsulated drug with release of a significant fraction of payload into release medium within a short period, both in vitro and in vivo, remains a challenge for translation. Such unpredictable and uncontrolled release is often undesirable, especially from the perspective of developing sustained-release formulations. Moreover, a brisk release of the payload upsets optimal release kinetics. This account strives toward understanding burst release noticed in nanocarriers and investigates its causes. Various mathematical models to explain such untimely release were also examined, including their strengths and weaknesses. Finally, the account revisits current techniques of limiting burst release from nanocarriers and prioritizes future directions that harbor potential of fruitful translation by reducing such occurrences.

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Local Delivery System Using Thermosensitive Hydrogel and Drug Loading Microspheres for Cartilage Repairing

Advanced Materials Research ◽

10.4028/www.scientific.net/amr.898.300 ◽

2014 ◽

Vol 898 ◽

pp. 300-303 ◽

Cited By ~ 1

Author(s):

Lei Wang ◽

Gang Wu

Keyword(s):

Drug Release ◽

Delivery System ◽

Ring Opening ◽

Drug Loading ◽

Local Drug Delivery ◽

Burst Release ◽

Transition Diagram ◽

Thermosensitive Hydrogel ◽

Local Drug Delivery System

A local drug delivery system constituted by hybrid microsphere/thermosensitive hydrogel was fabricated for Osteoarthritis (OA) therapy in the research. The hydrogel were synthesized by ring-opening copolymerization. Microsphere was fabricated by O/W emulsion and solution evaporation method. The properties of the products were characterized by 1HNMR, FTIR and phase transition diagram. The microsphere/hydrogel was prepared for in vitro drug release research. The results showed microsphere/hydrogel hybrid system can alleviate initial burst release. After 650 hours, only 60 percent of the drugs were released. Kinetics research implied the drug release is controlled by diffusion/erosion mechanism.

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Development of Bioadhesive Chitosan Superporous Hydrogel Composite Particles Based Intestinal Drug Delivery System

BioMed Research International ◽

10.1155/2013/563651 ◽

2013 ◽

Vol 2013 ◽

pp. 1-10 ◽

Cited By ~ 8

Author(s):

Hitesh Chavda ◽

Ishan Modhia ◽

Anant Mehta ◽

Rupal Patel ◽

Chhagan Patel

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Drug Delivery System ◽

Delivery System ◽

Drug Transport ◽

Release Kinetics ◽

Hydrogel Composite ◽

Intestinal Delivery ◽

Superporous Hydrogel

Bioadhesive superporous hydrogel composite (SPHC) particles were developed for an intestinal delivery of metoprolol succinate and characterized for density, porosity, swelling, morphology, and bioadhesion studies. Chitosan and HPMC were used as bioadhesive and release retardant polymers, respectively. A 32full factorial design was applied to optimize the concentration of chitosan and HPMC. The drug loaded bioadhesive SPHC particles were filled in capsule, and the capsule was coated with cellulose acetate phthalate and evaluated for drug content,in vitrodrug release, and stability studies. To ascertain the drug release kinetics, the drug release profiles were fitted for mathematical models. The prepared system remains bioadhesive up to eight hours in intestine and showed Hixson-Crowell release with anomalous nonfickian type of drug transport. The application of SPHC polymer particles as a biomaterial carrier opens a new insight into bioadhesive drug delivery system and could be a future platform for other molecules for intestinal delivery.

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Floating microspheres of Miglitol as gastro retentive drug delivery system: 32 full factorial design and in vitro evaluation

10.21203/rs.3.rs-826326/v1 ◽

2021 ◽

Author(s):

Cheran K ◽

Udaykumar B Bolmal ◽

Archana S Patil ◽

Umashri A Kokatanur ◽

Rajashree S Masareddy

Keyword(s):

Drug Delivery ◽

Particle Size ◽

Drug Release ◽

Drug Delivery System ◽

Delivery System ◽

Polymer Concentration ◽

Entrapment Efficiency ◽

Drug Entrapment Efficiency ◽

Gastro Retentive

Abstract Background: The goal of this study was to develop a gastro retentive floating drug delivery system that would improve site specific activity, patient compliance and therapeutic efficacy.Methodology: Floating microspheres of Miglitol were formulated by double emulsion method using ethyl cellulose and eudragit E100 different weight ratio and PVA as an emulsifier. It has been prepared with respect quantity of polymer concentration and stirring speed to evaluate for % buoyancy, drug entrapment efficiency, particle size drug release rate. Result: The percent of buoyancy, drug entrapment efficiency, particle size, and percentage yield were increased with increase the polymer mixture concentration. Among all formulation batches, F6 showed acceptable results drug entrapment efficiency (86.57%) and buoyancy (94.25%). F10 formulation was prepared to check the predicted and actual factors and compared with optimized formulation F6. The drug release was increased as the polymer concentration was decrease. The kinetic model zero order had the highest regression coefficient value, it was described as a sustained release dosage form. According to ICH guideline accelerated stability studies of F6 and F10 formulations were conducted for 90 days. After 90 days buoyancy and in vitro drug release was performed and the results were F6 and F10 buoyancy was found to be 88.21%, 87.22% and in vitro drug release was found to be 62.87%, 63.51%. Conclusion: The present study, showed compatibility of drug with polymers by FTIR in formulation. Floating microsphere of Miglitol was prepared by double emulsion technique. The F6 Miglitol floating microsphere was optimized formulation demonstrated with excellent drug entrapment performance (86.57%), good floating behaviour (94.25%), and the largest particle size (670µm). The present study concludes that floating based gastro retentive delivery system of Miglitol microspheres has a safe and effective drug delivery system with increased therapeutic efficacy and a longer duration of action.

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Kinetics of drug release from a biodegradable local drug delivery system and its effect on Porphyromonas gingivalis isolates: An in vitro study

Journal of Indian Society of Periodontology ◽

10.4103/0972-124x.118311 ◽

2013 ◽

Vol 17 (4) ◽

pp. 429 ◽

Cited By ~ 1

Author(s):

Ranganathan Vijayalashmi ◽

SabithaManhalore Ravindranath ◽

NadathurDoraiswamy Jayakumar ◽

Padmalatha ◽

SheejaH Vargheese ◽

...

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Drug Delivery System ◽

Porphyromonas Gingivalis ◽

Delivery System ◽

In Vitro Study ◽

Local Drug Delivery ◽

Local Drug Delivery System ◽

Kinetics Of

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PREPARATION AND CHARACTERIZATION OF SELF NANO EMULSIFYING DRUG DELIVERY SYSTEM CONTAINING ANTI-HYPERTENSIVE DRUG’’

Journal of Biomedical and Pharmaceutical Research ◽

10.32553/jbpr.v9i4.777 ◽

2020 ◽

Vol 9 (4) ◽

Author(s):

Anukumar E ◽

Nagaraja T S ◽

Yogananda R ◽

Bharathi D R

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Drug Delivery System ◽

Delivery System ◽

Release Kinetics ◽

Stability Studies ◽

In Vitro Drug Release ◽

Hypertensive Drug

The present work is to prepare and characterization of self nano emulsifying drug delivery system containing Anti-hypertensive drug. Losartan is a competitive antagonist and inverse agonist of angiotensin 2 receptor. The SNEDDS is prepared by Sonication method using a components of SPAN 60/Eudragit RS 100 as a surfactant, PVA as a Co-surfactant, Iso propyl alcohol as a solvent and DCM as a co-solvent. The prepared SNEDDS was evaluated for Fourier transform infrared spectroscopy, Surface morphology, particle size, zeta potential, drug entrapment efficiency, visual assessment, self-emulsification time, Robustness to dilution, in-vitro drug release and short term stability studies. The in-vitro drug release data of all the formulations were found to be zero order over a period of 24 h and Formulation F7 shows good results for the drug release kinetics as controlled release. The stability studies data was found that there was no such difference in drug EE and in-vitro drug release.

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Development, Characterization, and In Vitro Evaluation of Resveratrol-Loaded Poly-(ε-caprolactone) Microcapsules Prepared by Ultrasonic Atomization for Intra-Articular Administration

Pharmaceutics ◽

10.3390/pharmaceutics11060249 ◽

2019 ◽

Vol 11 (6) ◽

pp. 249 ◽

Cited By ~ 4

Author(s):

Asteria Luzardo-Álvarez ◽

Iván Lamela-Gómez ◽

Francisco Otero-Espinar ◽

José Blanco-Méndez

Keyword(s):

Drug Delivery ◽

Particle Size ◽

Drug Delivery System ◽

Delivery System ◽

Inflammatory Responses ◽

Polymer Concentration ◽

Joint Disease ◽

Oral Drug ◽

Ultrasonic Atomization

Intra-articular administration of drugs to the joint in the treatment of joint disease has the potential to minimize the systemic bioavailability and the usual side-effects associated with oral drug administration. In this work, a drug delivery system is proposed to achieve an anti-inflammatory local effect using resveratrol (RSV). This study aims to develop microcapsules made of poly-(ε-caprolactone) (PCL) by ultrasonic atomization to preserve the antioxidant activity of RSV, to prevent its degradation and to suppress the inflammatory response in activated RAW 264.7 macrophages. An experimental design was performed to build a mathematical model that could estimate the effect of nozzle power and polymer concentration on particle size and encapsulation efficiency. RSV-loaded microcapsules showed adequate morphology, particle size, and loading efficiency properties. RSV formulations exhibited negligible cytotoxicity and an efficient amelioration of inflammatory responses, in terms of Nitric Oxide (NO), ROS (Reactive Oxygen Species), and lipid peroxidation in macrophages. Thus, RSV-loaded microcapsules merit consideration as a drug delivery system suitable for intra-articular administration in inflammatory disorders affecting the joint.

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