scholarly journals DEVELOPMENT AND EVALUATION OF ORAL SUSTAINED-RELEASE RANITIDINE DELIVERY SYSTEM BASED ON BACTERIAL NANOCELLULOSE MATERIAL PRODUCED BY KOMAGATAEIBACTER XYLINUS

2020 ◽  
pp. 48-55
Author(s):  
THANH XUAN NGUYEN ◽  
MUNG VAN PHAM ◽  
CUONG BA CAO
Keyword(s):  
Sustained Release ◽  
Delivery System ◽  
Culture Media ◽  
Release Kinetics ◽  
Release Mechanism ◽  
Burst Release ◽  
Bacterial Nanocellulose ◽  
Release System ◽  
Komagataeibacter Xylinus

Objective: The short biological half-life (2-3 h) and low bioavailability (50 %) of ranitidine (RAN) following oral administration favor the development of a controlled release system. This study was aimed to develop and in vitro evaluate oral sustained-release RAN delivery system based on the bacterial nanocellulose material (BNM) produced by Komagataeibacter xylinus (K. xylinus) from selected culture media. Methods: BNMs are biosynthesized by K. xylinus in the standard medium (SM) and coconut water (CW). RAN was loaded in BNMs by the absorption method. The structural and physicochemical properties of BNMs and BNMs-RAN were evaluated via swelling behavior, FTIR, and FESEM techniques. Moreover, the effect of BNMs on RAN release profile and release kinetics was analyzed and evaluated. Results: The amount of loaded RAN or entrapment efficacy for BNM-CW is higher than for BNM-SM. The BNM-SM-RAN and BNM-CW-RAN exhibited a decreased initial burst release system followed by a prolonged RAN release up to 24 h in relation to the commercial tablets containing RAN. The RAN release from these formulations was found higher in the SGF medium than that of in SIF medium. RAN released from these formulations was found to follow the Korsmeyer-Peppas model and diffusion sustained drug release mechanism. The sustained release of RAN from BNM-SM-RAN was slower than for RAN from BNM-CW-RAN, but the mechanism of sustained RAN release was the same. Conclusion: Oral sustained-release RAN delivery system based on BNMs was successfully prepared and evaluated for various in vitro parameters. The biopolymers like BNM-SM and BNM-CW could be utilized to develop oral sustained RAN release dosage form.

scholarly journals Thermosensitive Chitosan Hydrogels Containing Polymeric Microspheres for Vaginal Drug Delivery

2017 ◽  
Vol 2017 ◽  
pp. 1-12 ◽  
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.

scholarly journals Design, Fabrication and Evaluation of Drug Release Kinetics from Aceclofenac Matrix Tablets using Hydroxypropyl Methyl Cellulose

1970 ◽  
Vol 8 (1) ◽  
pp. 23-30 ◽  
Author(s):  
Abul Kalam Lutful Kabir ◽  
Bishyajit Kumar Biswas ◽  
Abu Shara Shasur Rouf
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
Matrix Tablets ◽  
Angle Of Repose ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Drug Content ◽  
Compressibility Index

The objective of this study was to develop a sustained release matrix tablet of aceclofenac usinghydroxypropyl methylcellulose (HPMC K15M and HPMC K100M CR) in various proportions as release controllingfactor by direct compression method. The powders for tableting were evaluated for angle of repose, loose bulkdensity, tapped bulk density, compressibility index, total porosity and drug content etc. The tablets were subjected tothickness, weight variation test, drug content, hardness, friability and in vitro release studies. The in vitro dissolutionstudy was carried out for 24 hours using United States Pharmacopoeia (USP) 22 paddle-type dissolution apparatus inphosphate buffer (pH 7.4). The granules showed satisfactory flow properties, compressibility index and drug contentetc. All the tablets complied with pharmacopoeial specifications. The results of dissolution studies indicated that theformulations F-2 and F-3 could extend the drug release up to 24 hours. By comparing the dissolution profiles with themarketed product, it revealed that the formulations exhibited similar drug release profile. From this study, a decreasein release kinetics of the drug was observed when the polymer concentration was increased. Kinetic modeling of invitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport toanomalous type or non-Fickian transport, which was only dependent on the type and amount of polymer used. Thedrug release followed both diffusion and erosion mechanism in all cases. The drug release from these formulationswas satisfactory after 3 months storage in 40°C and 75% RH. Besides, this study explored the optimum concentrationand effect of polymer(s) on acelofenac release pattern from the tablet matrix for 24 hour period.Key words: Aceclofenac; sustained release; hydrophillic matrix; HPMC; direct compression.DOI: 10.3329/dujps.v8i1.5332Dhaka Univ. J. Pharm. Sci. 8(1): 23-30, 2009 (June)

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

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.

scholarly journals Evaluation of in vitro release kinetics of Capsaicin-loaded chitosan nanoparticles using DDSolver

2020 ◽  
Vol 11 (3) ◽  
pp. 4555-4559
Author(s):  
Narissara Kulpreechanan ◽  
Feuangthit Niyamissara Sorasitthiyanukarn
Keyword(s):  
Gastrointestinal Tract ◽  
Sustained Release ◽  
Release Kinetics ◽  
Chitosan Nanoparticles ◽  
Circulatory System ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Release Study ◽  
Kinetics Of

The present aim is to evaluate the release profile and its release kinetics of encapsulated capsaicin from chitosan nanoparticles using the software DDSolver. The release study was performed by using a dialysis technique in PBS solutions with different pHs (1.2, 6.8 and 7.4) to mimics the different gastrointestinal tract and circulatory system pH ranges as a releasing medium. The nanoparticles were prepared using o/w emulsification and ionotropic gelation technique under optimal condition obtained from response surface methodology (RSM) design as described in our previous study. These nanoparticles were around 180 nm in average hydrodynamic size and encapsulation efficiency percentage around 70%, respectively. In vitro drug release study suggested that the chitosan nanoparticles can potentially use to controlled and sustained release of capsaicin over at least 96. The kinetic release analysis results by DDSolver software indicated that Weibull model was suggested to be the best dynamic models with highest R2adjusted and model selection criteria (MSC) and lowest Akaike information criterion (AIC), respectively, for capsaicin loaded chitosan nanoparticles. The release mechanism of capsaicin from nanoparticles was found to be Fickian diffusion. The results suggest that the chitosan nanoparticles can be applied for the controlled and sustained release of capsaicin in the gastrointestinal tract and circulatory system.

scholarly journals Formulation and Evaluation of Polymer Effect on In-Vitro Kinetics of Sustained Release Matrix Tablets of Carvedilol Using Model Dependent Methods

2013 ◽  
Vol 2 (2) ◽  
pp. 70-79
Author(s):  
Umme Rahela ◽  
Md Mizanur Rahman Moghal ◽  
Sayed Masudur Rahman Dewan ◽  
Mohammad Nurul Amin
Keyword(s):  
Sustained Release ◽  
Drug Product ◽  
Release Kinetics ◽  
Matrix Tablets ◽  
Release Mechanism ◽  
Physical Parameters ◽  
Kinetics Of ◽  
In Vitro Kinetics ◽  
Polymeric Effect

The present study was designed to evaluate the polymeric effect of METHOCEL K15MCR on the sustained release drug product of Carvedilol. Carvedilol matrix tablets were formulated by direct compression method using METHOCEL K15MCR polymer in various percentages. Physical parameters were tested and the dissolution procedure was performed by using USP (II) paddle method for eight hours to examine the release kinetics. In the study, METHOCEL K15MCR polymer was found to cause the strong retardation of the drug release. The release mechanism was explored and explained with zero order, first order, Higuchi and Korsmeyer-Peppas equations. In the context, it can be suggested with a satisfactory result that this sustained release Carvedilol tablets can be marketed to treat patient ensuring proper healthcare. DOI: http://dx.doi.org/10.3329/ijpls.v2i2.15452 International Journal of Pharmaceutical and Life Sciences Vol.2(2) 2013: 70-79

scholarly journals Development of Salbutamol Sulphate Sustained Release Pellets Using Acrylic Polymer and Polyvinyl Acetate Polymer and Evaluation of In vitro Release Kinetics

1970 ◽  
Vol 9 (2) ◽  
pp. 109-118 ◽  
Author(s):  
Saki Sultana ◽  
Ishtiaq Ahmed ◽  
Muhammad R Islam ◽  
Md Habibur Rahman
Keyword(s):  
Sustained Release ◽  
Polyvinyl Acetate ◽  
Release Kinetics ◽  
Aqueous Dispersion ◽  
Release Mechanism ◽  
Scanning Electron Micrographs ◽  
Acrylic Polymer ◽  
Salbutamol Sulphate ◽  
Temperature Scanning

The nuclei of sustained-release pellets of salbutamol sulphate were prepared using extrusionspheronization technique followed by coating with the aqueous dispersion of methacrylic acid esters (Eudragit RS® 30 D) and commercial aqueous polyvinyl acetate dispersion (30% dispersion) (Kollicoat SR® 30 D). The coating polymers were applied to obtain a theoretical polymer load of 5%, 10%, 15%, 20% & 25 %( w/w) on the nuclei. Invitro dissolution studies of the coated pellets were performed in a USP paddle apparatus (type-2). Dissolution media was distilled water (500 ml), paddle speed was 50 rpm and it was preformed for 8 hours at 37°C (±0.5°C) temperature. Scanning Electron Micrographs (SEMs) of the nuclei & coated pellets were taken to study their surface morphology. The kinetics of the dissolution process was determined by analyzing the dissolution data using zeroorder, first order, Higuchi and Korsmeyer equations. The kinetic modeling of the dissolution profiles revealed that drug release mechanism ranged from diffusion controlled or Fickian transport to anomalous type or non-Fickian transport. T50% (MDT) and T90% values were calculated for each formulation. The higher MDT values were obtained with Eudragit® RS 30D where as Kollicoat® SR 30D showed comparatively low MDT values. MDT values were also increased with increasing polymer load on the nuclei. Key words: Salbutamol sulphate; Pellet; Aqueous dispersion; Eudragit® RS 30 D; Kollicoat® SR 30D; Extrusion spheronization; MDT. DOI: http://dx.doi.org/10.3329/dujps.v9i2.7895 Dhaka Univ. J. Pharm. Sci. 9(2): 109-118, 2010 (December)

scholarly journals A novel BMP-2–loaded hydroxyapatite/beta-tricalcium phosphate microsphere/hydrogel composite for bone regeneration

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Daisuke Tateiwa ◽  
Shinichi Nakagawa ◽  
Hiroyuki Tsukazaki ◽  
Rintaro Okada ◽  
Joe Kodama ◽  
...  
Keyword(s):  
Sustained Release ◽  
Bone Regeneration ◽  
Tricalcium Phosphate ◽  
Release Kinetics ◽  
Poloxamer 407 ◽  
Enzyme Linked Immunosorbent Assay ◽  
Burst Release ◽  
Beta Tricalcium Phosphate

AbstractAlthough bone morphogenetic protein (BMP) has potent osteoinductivity, the potential adverse events attributed to its burst release prevent its widespread clinical application. Therefore, there is a strong need for BMP delivery systems that maximize osteoinductivity while preventing adverse effects. We evaluated the bone-regenerating potential of NOVOSIS putty (NP), a novel composite combining hydroxyapatite, beta-tricalcium phosphate microsphere/poloxamer 407-based hydrogel, and recombinant human (rh) BMP-2. In vitro assessment of release kinetics by enzyme-linked immunosorbent assay demonstrated sustained release of rhBMP-2 from NP and burst release from collagen sponge (CS), and in vivo assessment of release kinetics by longitudinal tracking of fluorescently labeled rhBMP-2 showed a longer biological half-life of rhBMP-2 with NP than with CS. Furthermore, osteogenic gene expression in MC3T3-E1 cells was significantly higher after co-culture with NP than after co-culture with CS, suggesting that the sustained release of rhBMP-2 from NP effectively contributed to the differentiation of osteoblasts. In a rat spinal fusion model, the volume and quality of newly formed bone was higher in the NP group than in the CS group. Use of NP results in efficient bone regeneration through sustained release of rhBMP-2 and improves the quality of BMP-induced bone.

Bentonite nanoclay-based drug-delivery systems for treating melanoma

Clay Minerals ◽  
2018 ◽  
Vol 53 (1) ◽  
pp. 53-63 ◽  
Author(s):  
Faezeh Hosseini ◽  
Farzaneh Hosseini ◽  
Seyyed Mehdi Jafari ◽  
Azade Taheri
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Burst Release ◽  
Normal Tissues ◽  
Release Pattern

ABSTRACTLocal chemotherapy with biocompatible drug-delivery systems prolongs survival in patients. Due to the biocompatibility and high loading capacity, bentonite nanoclay is a good candidate for the fabrication of drug-delivery vehicles. In this study, doxorubicin-bentonite nanoclay complex (DOX-Bent complex) was prepared for the first time as a sustained-release drug-delivery system for intratumoural chemotherapy of melanoma. An efficient loading of DOX on 1 mg of bentonite nanoclay as high as 994.45 ± 4.9 µg was obtained at a 30:1 DOX:bentonite nanoclay mass ratio. The DOX-Bent complex showed a low initial burst release of DOX in the first 24 h of release, followed by a sustained-release pattern for 21 days. The cumulativein vitrorelease of DOX from the DOX-Bent complex at pHs 6.5 and 7.4 revealed that the DOX-Bent complex can distinguish between tumour and normal tissues and express specific drug release at the tumour site. The results of cytotoxicity experiments indicated that the release pattern of DOX can supply sufficient DOX to inhibit growth of the melanoma cancer cell with an IC50 of 0.29 ± 0.07 µg/mL. It is thus suggested that the DOX-Bent complex be introduced as a drug-delivery system for effective local cancer therapy.

scholarly journals Investigation of the Release Mechanism and Mould Resistance of Citral-Loaded Bamboo Strips

Polymers ◽  
2021 ◽  
Vol 13 (19) ◽  
pp. 3314
Author(s):  
Rui Peng ◽  
Jingjing Zhang ◽  
Chungui Du ◽  
Qi Li ◽  
Ailian Hu ◽  
...  
Keyword(s):  
Sustained Release ◽  
Release Kinetics ◽  
Drug Loading ◽  
Trichoderma Viride ◽  
Release Mechanism ◽  
Control Effect ◽  
External Temperature ◽  
First Order ◽  
Release System ◽  
Optimal Drug

In the present study, the sustained-release system loading citral was synthesised by using PNIPAm nanohydrogel as a carrier and analysed its drug-release kinetics and mechanism. Four release models, namely zero-order, first-order, Higuchi, and Peppas, were employed to fit the experimental data, and the underlying action mechanism was analysed. The optimised system was applied to treat a bamboo mould, followed by assessment of the mould-proof performance. Our experimental results revealed that the release kinetics equation of the system conformed to the first order; the higher the external temperature, the better the match was. In the release process, PNIPAm demonstrated a good protection and sustained-release effect on citral. Under the pressure of 0.5 MPa, immersion time of 120 min, and the system concentration ratio of 1, the optimal drug-loading parameters were obtained using the slow-release system with the best release parameters. Compared to the other conditions, bamboos treated with pressure impregnation demonstrated a better control effect on bamboo mould, while the control effect on Penicillium citrinum, Trichoderma viride, Aspergillus niger, and mixed mould was 100% after 28 days. Moreover, the structure and colour of bamboo remained unchanged during the entire process of mould control.

scholarly journals Preparation and in vitro release kinetics of ivermectin sustained-release bolus optimized by response surface methodology

PeerJ ◽  
2018 ◽  
Vol 6 ◽  
pp. e5418 ◽  
Author(s):  
Xiangchun Ruan ◽  
Xiuge Gao ◽  
Ying Gao ◽  
Lin Peng ◽  
Hui Ji ◽  
...  
Keyword(s):  
Response Surface Methodology ◽  
Sustained Release ◽  
Response Surface ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Information Criterion ◽  
Quadratic Model ◽  
Dissolution Time ◽  
Release Mechanism

Sustained-release formulations of ivermectin (IVM) are useful for controlling parasitic diseases in animals. In this work, an IVM bolus made from microcrystalline cellulose (MCC), starch and low-substituted hydroxypropyl cellulose (LS-HPC) was optimized by response surface methodology. The bolus was dissolved in a cup containing 900 mL of dissolution medium at 39.5 °C, under with stirring at 100 rpm. A quadratic model was formulated using analysis of variance according to the dissolution time. The optimized formulation of the bolus contained 8% MCC, 0.5% starch, and 0.25% LS-HPC. The length, width, and height of the prepared IVM bolus were 28.12 ± 0.14, 16.1 ± 0.13, and 13.03 ± 0.05 mm, respectively. The bolus weighed 11.4842 ± 0.1675 g (with a density of 1.95 g/cm3) and contained 458.26 ± 6.68 mg of IVM. It exhibited in vitro sustained-release for over 60 days, with a cumulative amount and percentage of released IVM of 423.72 ± 5.48 mg and 92.52 ± 1.20%, respectively. The Korsmeyer–Peppas model provided the best fit to the dissolution release kinetics, exhibiting anR2value close to 1 and the lowest Akaike Information Criterion among different models. The parametern(0.5180) of the Korsmeyer–Peppas model was between 0.45 and 0.89. It was demonstrated that the release mechanism of the IVM bolus followed a diffusive erosion style.

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