scholarly journals Recent Progress in Drug Release Testing Methods of Biopolymeric Particulate System

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1313
Author(s):  
Yejin Kim ◽  
Eun Ji Park ◽  
Tae Wan Kim ◽  
Dong Hee Na

Biopolymeric microparticles have been widely used for long-term release formulations of short half-life chemicals or synthetic peptides. Characterization of the drug release from microparticles is important to ensure product quality and desired pharmacological effect. However, there is no official method for long-term release parenteral dosage forms. Much work has been done to develop methods for in vitro drug release testing, generally grouped into three major categories: sample and separate, dialysis membrane, and continuous flow (flow-through cell) methods. In vitro drug release testing also plays an important role in providing insight into the in vivo performance of a product. In vitro release test with in vivo relevance can reduce the cost of conducting in vivo studies and accelerate drug product development. Therefore, investigation of the in vitro–in vivo correlation (IVIVC) is increasingly becoming an essential part of particulate formulation development. This review summarizes the principles of the in vitro release testing methods of biopolymeric particulate system with the recent research articles and discusses their characteristics including IVIVC, accelerated release testing methods, and stability of encapsulated drugs.

2018 ◽  
Vol 8 (5-s) ◽  
pp. 235-239
Author(s):  
NILESH M MAHAJAN ◽  
Kalyanee Wanaskar ◽  
Yogesh Bhutada ◽  
Raju Thenge ◽  
Vaibhav Adhao

The aim of present study is to formulate and evaluate extended release matrix tablet of Nateglinide by direct compression method using different polymer like HPMC K4 and HPMC K15. Matrix tablet of nateglidine were prepared in combination with the polymer HPMC K4, HPMC K15, along with the excipients and the formulations were evaluated for tablet properties and in vitro drug release studies. Nateglinide matrix tablet prepared by using polymer such as HPMC K4 and HPMC K15,  it was found that HPMC K15 having higher viscosity as compare to HPMC K4 therefore different concentration of polymer were studied to extend the drug release up to 12 h. The tablets of Nateglinide prepared by direct compression had acceptable physical characteristics and satisfactory drug release. The study demonstrated that as far as the formulations were concerned, the selected polymers proved to have an acceptable flexibility in terms of in-vitro release profile. In present the study the percent drug release for optimize batch was found to 94.62%.  Hence it can be conclude that Nateglinide extended release matrix tablet can prepared by using HPMC. The swollen tablet also maintains its physical integrity during the drug release study Keywords: Tablet, in-vitro drug release, Nateglinide, HPMC


Author(s):  
AMRIN SHAIKH ◽  
PRASHANT BHIDE ◽  
REESHWA NACHINOLKAR

Objective: The aim of the present investigation was to design gels for the topical delivery of celecoxib and evaluate with an aim to increase its penetration through the skin and thereby its flux. Method: The solubility of celecoxib is shown to be increased by preparing solid dispersions (SDs) using carriers such as mannitol, polyvinylpyrrolidone (PVP-K30), polyethylene glycol (PEG) 6000 and urea by solvent evaporation, fusion, and coevaporation methods. In vitro release profile of all SD was comparatively evaluated and studied against the pure drug. The prepared SD was subjected for percent practical yield, drug content, infrared spectroscopy, differential scanning calorimetry analysis, X-ray diffraction studies, and scanning electron microscopy (SEM) imaging. The celecoxib gel was prepared using hydroxypropyl methyl cellulose (HPMC) and Carbopol containing a permeation enhancer dimethyl sulfoxide (DMSO) at different proportions and evaluated for drug content, pH, viscosity, spreadability, extrudability, stability, and in vitro drug release. Results: Faster dissolution rate was exhibited by SD containing 1:5 ratio of celecoxib: PVP K-30 prepared by coevaporation method. In vitro drug release of celecoxib, gels revealed that formulation with HPMC has higher drug release as compared to Carbopol. Conclusion: The increase in dissolution rate for SD is observed in the following order of PVP K-30>urea>mannitol>PEG 6000. The CPD5 gel containing a SD CP5 and 20% DMSO showed the best in vitro release 74.13% at the end of 6 h.


Author(s):  
Raditya Iswandana ◽  
Kurnia Sari Setio Putri ◽  
Cindy Espreancelly Sandiata ◽  
Sisilia Triani ◽  
Santi Purna Sari ◽  
...  

Objectives Pectin, a natural polysaccharide, can be used as colon targeted drug delivery systems. Ionotropic gelation of pectin in the presence of certain divalent cations, such as calcium ions, protects drugs by producing insoluble hydrogels that can be used as a colon-targeted drug delivery carrier. In this study, calcium pectinate beads containing tetrandrine were made and were evaluated for in-vitro drug release and in-vivo study.Methods: Calcium pectinate beads were prepared by ionic gelation method with varied calcium chloride concentration (5%, 10%, and 15%). The best formula was coated with pH sensitive polymers, i.e. Eudragit L100-55, Eudragit L100, HPMCP (Hydroxypropylmethyl Cellulose Phthalate) HP-55 or CAP (Cellulose Acetate Phthalate).Results: Characterization results showed that the beads produced were quite spherical and have yellow-brownish color. After the coating process, beads were used in in-vitro drug release and targeted test. From in-vitro release study, beads coated with Eudragit L100 10% has shown good colon targeted dosage form with percent cumulative release 57.87%. This result also confirmed with the in-vivo test. Beads which were coated by Eudragit L100 10% could be found in the rat intestine.Conclusion: Formula 1 (5% calcium chloride concentration) was chosen as the best beads characterization. Formula 1C (5% beads coated with 10% Eudragit L100) showed an optimal protection from gastric acid in the in-vitro release study and able to deliver the beads to the intestine in the in-vivo targeted test.


2014 ◽  
Vol 475 (1-2) ◽  
pp. 393-400 ◽  
Author(s):  
Jacqueline M. Morais ◽  
Diane J. Burgess

Author(s):  
Naga sai divya K ◽  
T Malyadri ◽  
Ch.saibabu

The purpose of the present study was to develop and optimize the emulgel system for Luliconazole using different types of gelling agents: HPMCK15M, Carbopol 940, and Xanthan Gum. The prepared emulgels were evaluated in terms of appearance, pH, spreadability, viscosity, drug content, and in-vitro drug release. In-vitro release study demonstrated diffusion-controlled release of Luliconazole from formulation up to 12 hours. The drug release profile exhibited zero-order kinetics. All the prepared emulgels showed acceptable physical properties concerning color, homogeneity, consistency, spreadability, and higher drug release. In the case of all evaluation parameters, carbopol based formulation showed better properties so, as a general conclusion, it was suggested that the Luliconazole emulgel formulation prepared with carbopol (F6) was the formula of choice.


2020 ◽  
Vol 88 (1) ◽  
pp. 6
Author(s):  
Potiwa Purazi ◽  
Seeprarani Rath ◽  
Ashmita Ramanah ◽  
Isadore Kanfer

In vitro release testing (IVRT) provides an efficient method for the evaluation of drug release from semi-solid formulations. The aim of this research was to develop and validate a discriminatory IVRT system using vertical diffusion cells (VDCs) to assess generic topical products containing miconazole nitrate (MCZ). A comprehensive approach addressing all essential suitability criteria supporting the reliability of IVRT results was applied. These include mechanical validation of the VDCs, a performance verification test (PVT), validation of the analytical method (HPLC) used to quantify the drug release and validation of the IVRT method to confirm its precision, reproducibility, discriminatory ability, and robustness. Two marketed generic products were tested and assessed in accordance with the acceptance criteria for “sameness” in the FDA’s SUPAC-SS guidance which requires that the 90% confidence interval (CI) should fall within the limits of 75%–133.33%. One product was found to be in vitro equivalent to the reference product whereas the other was not. The results confirmed the suitability of the IVRT method to accurately measure the release of MCZ from topical cream products and, importantly, demonstrated the necessary discriminatory ability to assess “sameness”/differences of dermatological creams containing MCZ. Furthermore, the developed IVRT method was able to detect differences between formulations, which may be attributed to qualitative (Q1) and quantitative (Q2) properties and the microstructure and arrangement of matter (Q3).


Author(s):  
Chandra Sekhar Kolli ◽  
Ramesh Gannu ◽  
Vamshi Vishnu Yamsani ◽  
Kishan V ◽  
Madhsudan Rao Yamsani

The aim of this investigation was to develop and evaluate mucoadhesive buccal patches of prochlorperazine (PCPZ). Permeation of PCPZ was calculated in vitro using porcine buccal membrane. Buccal formulations were developed by solvent-casting technique using hydroxy propylmethyl cellulose (HPMC) as mucoadhesive polymer. The patches were evaluated for in vitro release, moisture absorption and mechanical properties. The optimized formulation, based on in vitro release and moisture absorption studies, was subjected for bioadhesion studies using porcine buccal membrane. In vitro flux of PCPZ was calculated to be 2.14 ± 0.01 µg. h–1.cm–2 and buccal absorption was also demonstrated in vivo in human volunteers.             In vitro drug release and moisture absorbed was governed by HPMC content. Increasing concentration of HPMC delayed the drug release. All formulations followed Zero order release kinetics whereas the release pattern was non-Fickian. The mechanical properties, tensile strength (10.28 ± 2.27 kg mm–2 for formulation P3) and elongation at break reveal that the formulations were found to be strong but not brittle. The peak detachment force and work of adhesion for formulation P3 were 0.68 ± 0.15 N and 0.14 ± 0.08 mJ, respectively. The results indicate that suitable bioadhesive buccal patches of PCPZ with desired permeability and suitable mechanical properties could be prepared


Fig. 12 Scanning electron micrograph of D.L-PLA nanoparticles loaded with CGP 57813. (Ref. 51.) scanning force microscopy (also called atomic force microscopy), enable the visualiza-tion of nanoparticles at atmospheric pressure without gold coating [12,64]. Neverthe-less, the resolution obtained with these new tools is still lower than that with SEM. For size determination, transmission electron microscopy is not as widely used as PCS and SEM, but it is still a powerful method for determining the morphology of particles. With this technique, Fessi et al. [42] estimated the wall thickness of PLA nanocapsules. Krause et al. [18] described the highly porous structure of PLA nano-spheres prepared by the emulsion-evaporation procedure. VIII. IN VITRO RELEASE STUDIES In vitro release studies should in principle be useful for quality control as well as for the prediction of in vivo kinetics. Unfortunately, due to the very small size of the par-ticles, the release rate observed in vivo can differ greatly from the release obtained in a buffer solution. However, in vitro release studies remain very useful for quality control as well as for evaluation of the influence of process parameters on the release rate of active compounds. In vitro drug release from microdispersed systems has been exten-sively reviewed by Washington [65]. Depending on the type of polyester, drug release from nanoparticles can take place through several processes, of which the following appear to be the most important: (1) The drug may diffuse out of the carrier through the solid matrix; to allow complete release from the carriers, (the concentration of drug in the release medium should re-main infinitely low, which condition is known as sink condition); (2) The solvent may penetrate the nanoparticles and dissolve the drug, which then diffuses out into the re-lease medium. Depending on the physico-chemical characteristics of the particles, wa-ter can enter the particles through narrow pores or by hydration. Once the drug is dis-solved, the drug diffuses out of the particles. Here again, since diffusion is driving the

1998 ◽  
pp. 204-216

Author(s):  
Surendra Singh Saurabh ◽  
Roshan Issarani ◽  
Nagori Bp

Objective: In the present dissertation work, the aim was to prepare self-emulsifying drug delivery systems (SEDDS) of etoricoxib to improve its solubility with a view to enhance its oral bioavailability.Methods: The prepared SEDDS was the concentrate of drug, oil, surfactants, and cosurfactant. The formulation was evaluated for various tests such as solubility, globule size, thermodynamic stability study, pH determination, ease of dispersibility, uniformity index, drug content, in-vitro release study, and in-vitro permeation study.Results: The optimized formulation F6 showed drug release (79.21±2.73%), droplet size (0.546 μm). In vitro drug release of the F6 was highly significant (p<0.05) as compared to the plain drug.Conclusion: All formulations of etoricoxib SEDDS were showed faster dissolution than plain drug (p<0.05), mean bioavailability of etoricoxib increase in respect to the plain drug. The F6 can be further used for the preparation of various solid SEDDS formulations.


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