Modified drug release of poloxamer matrix by including water-soluble and water-insoluble polymer

Humans have taken advantage of the adaptability of polymers for centuries in the form of resins, gums tars, and oils. However, it was not until the industrial revolution that the modern polymer industry began to develop. Polymers represent an important constituent of pharmaceutical dosage forms. Polymers have played vital roles in the formulation of pharmaceutical products. Polymers have been used as a major tool to manage the drug release rate from the formulations. Synthetic and natural-based polymers have found their way into the biomedical and pharmaceutical industries. Synthetic and Natural polymers can be produced with a broad range of strength, heat resistance, density, stiffness and even price. By constant research into the science and applications of polymers, they are playing an ever-increasing role in society. Diverse applications of polymers in the present pharmaceutical field are for controlled drug release. Based on solubility pharmaceutical polymers can be classified as water-soluble and water-insoluble. In general, the desirable polymer properties in pharmaceutical applications are film forming, adhesion, gelling, thickening, pH-dependent solubility and taste masking. General pharmaceutical applications of polymers in various pharmaceutical formulations are also discussed

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NANO-SIZED SOLID DISPERSION OF A POORLY WATER-SOLUBLE DRUG

Journal of Medicine and Pharmacy ◽

10.34071/jmp.2012.5.4 ◽

2012 ◽

pp. 31-35

Author(s):

Truong Dinh Thao Tran ◽

Ha Lien Phuong Tran ◽

Nghia Khanh Tran ◽

Van Toi Vo

Keyword(s):

Drug Release ◽

Droplet Size ◽

Solid Dispersion ◽

Water Soluble ◽

Drug Dissolution ◽

Dissolution Enhancement ◽

Particle Size Reduction ◽

Water Soluble Drug ◽

Poorly Water Soluble ◽

Poorly Water Soluble Drug

Purposes: Aims of this study are dissolution enhancement of a poorly water-soluble drug by nano-sized solid dispersion and investigation of machenism of drug release from the solid dispersion. A drug for osteoporosis treatment was used as the model drug in the study. Methods: melting method was used to prepare the solid dispersion. Drug dissolution rate was investigated at pH 1.2 and pH 6.8. Drug crystallinity was studied using differential scanning calorimetric and powder X-ray diffraction. In addition, droplet size and contact angle of drug were determined to elucidate mechanism of drug release. Results: Drug dissolution from the solid dispersion was significantly increased at pH 1.2 and pH 6.8 as compared to pure drug. Drug crystallinity was changed to partially amorphous. Also dissolution enhancement of drug was due to the improved wettability. The droplet size of drug was in the scale of nano-size when solid dispersion was dispersed in dissolution media. Conclusions: nano-sized solid dispersion in this research was a successful preparation to enhance bioavailability of a poorly water-soluble drug by mechanisms of crystal changes, particle size reduction and increase of wet property.

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Improved Dissolution Properties of Ketoconazole through Application of Liquisolid Techniques

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2015.8.4.9 ◽

2015 ◽

Vol 8 (4) ◽

pp. 3053-3059

Author(s):

Sudarshan Singh ◽

S S Shyale ◽

H G Sandip

Keyword(s):

Drug Release ◽

Immediate Release ◽

Water Soluble ◽

Wet Granulation ◽

Wetting Properties ◽

Enhanced Dissolution ◽

Water Soluble Drug ◽

Drug Concentrations ◽

Water Soluble Drugs ◽

Liquisolid Compacts

In present investigation liquisolid compact technique is investigated as a tool for enhanced dissolution of poorly water-soluble drug Ketoconazole. The liquisolid tablets were formulated with liquid medications, namely Propylene Glycol (PG) drug concentrations, 60% w/w, 70% w/w and 80% w/w. Avicel pH102 was used as a carrier material, Aerosil 200 as a coating material and Sodium starch glycollate as a super-disintegrant. Quality control tests, such as uniformity of tablet weight, uniformity of drug content, tablet hardness, friability test, disintegration and dissolution tests were performed to evaluate prepared tablets. For further confirmation of results the liquisolid compacts were evaluated by XRD and FTIR studies to prove that, solubility of Ketoconazole has been increased by liquisolid compact technique. From the results obtained, it was be speculated that such systems exhibit enhanced drug release profiles due to increased wetting properties and surface of drug available for dissolution. As liquisolid compacts demonstrated significantly higher drug release rates, in PG as compared to directly compressible tablets and conventional wet granulation, we lead to conclusion that it could be a promising strategy in improving the dissolution of poor water soluble drugs and formulating immediate release solid dosage forms.

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Formulation and Evaluation of Orally Disintegrating Tablets of Lamotrigine

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2015.8.2.11 ◽

2015 ◽

Vol 8 (2) ◽

pp. 2881-2888

Author(s):

Sudarshan Singh ◽

S S Shyale ◽

P Karade

Keyword(s):

Drug Release ◽

Water Soluble ◽

In Vitro Dissolution ◽

Disintegration Time ◽

Orally Disintegrating Tablet ◽

Drug Content ◽

Weight Variation ◽

Wetting Time ◽

Croscarmellose Sodium

The aim of this study was to design orally disintegrating tablet (ODT) of Lamotrigine. It is an Antiepileptic drug which is widely used in epilepsy. It is also used in simple and complex partial seizures and secondary generalized tonic-clonic seizures. It is poorly water soluble drug (0.46 mg/ml). Thus, an attempt was made to enhance the water solubility by complexation with β-cyclodextrin (1:1 molar ratios). The orally disintegrating tablet of lamotrigine was prepared by direct compression method using different concentration of superdisintegrants such as Sodium starch glycollate, croscarmellose sodium by sublimating agent such as camphor. The formulations were evaluated for weight variation, hardness, friability, drug content, wetting time, in vitro disintegration time and in vitro dissolution studies. The prepared tablets were characterized by Fourier transform infrared spectroscopy and differential scanning calorimetry. The disintegration time for the complexed tablets prepared by different concentration of superdisintegrants was found to be in range of 32.54 ± 0.50 to 55.12 ± 0.57 sec and wetting time of the formulations was found to be in range of 28.47 ± 0.67 to 52.19 ± 0.72 sec. All the formulation showed almost 100 percent of drug release within 15 min. Among all the formulation F6 and F7 prepared with 18% croscarmellose sodium and camphor shows faster drug release, respectively 10 min, F6 gives good result for disintegration time, drug release, wetting time and friability. Further formulations were subjected to stability testing for 30 days at temperature of 40 ± 5 ºC/75 ± 5 %RH. Tablets showed no appreciable changes with respect to physical appearance, drug content, disintegration time and dissolution profiles. Results were statistically analyzed by one-way ANOVA at a p < 0.05. It was found that, the data at any point of time are significant at p < 0.05.

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Mesoporous Silica Molecular Sieve based Nanocarriers: Transpiring Drug Dissolution Research

Current Pharmaceutical Design ◽

10.2174/1381612822666161026162005 ◽

2017 ◽

Vol 23 (3) ◽

pp. 467-480 ◽

Cited By ~ 8

Author(s):

Satyanarayan Pattnaik ◽

Kamla Pathak

Keyword(s):

Drug Release ◽

Mesoporous Silica ◽

Molecular Sieves ◽

Release Kinetics ◽

Drug Loading ◽

Scale Up ◽

Water Soluble ◽

Drug Dissolution ◽

Water Soluble Drugs ◽

Loading Methods

Background: Improvement of oral bioavailability through enhancement of dissolution for poorly soluble drugs has been a very promising approach. Recently, mesoporous silica based molecular sieves have demonstrated excellent properties to enhance the dissolution velocity of poorly water-soluble drugs. Description: Current research in this area is focused on investigating the factors influencing the drug release from these carriers, the kinetics of drug release and manufacturing approaches to scale-up production for commercial manufacture. Conclusion: This comprehensive review provides an overview of different methods adopted for synthesis of mesoporous materials, influence of processing factors on properties of these materials and drug loading methods. The drug release kinetics from mesoporous silica systems, the manufacturability and stability of these formulations are reviewed. Finally, the safety and biocompatibility issues related to these silica based materials are discussed.

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Formulation Development and Characterization of controlled release core in cup matrix tablets of venlafaxine HCl

Current Drug Therapy ◽

10.2174/1574885515666200331104440 ◽

2020 ◽

Vol 15 ◽

Author(s):

Balaji Maddiboyina ◽

Vikas Jhawat ◽

Gandhi Sivaraman ◽

Om Prakash Sunnapu ◽

Ramya Krishna Nakkala ◽

...

Keyword(s):

Controlled Release ◽

Drug Release ◽

Release Rate ◽

Zero Order ◽

Water Soluble ◽

Matrix Tablets ◽

Drug Dissolution ◽

Crystalline Cellulose ◽

Hydrophobic Polymers

Background: Venlafaxine HCl is a selective serotonin reuptake inhibitor which is given in the treatment of depression. The delivery of the drug at a controlled rate can be of great importance for prolonged effect. Objective: The objective was to prepare and optimize the controlled release core in cup matrix tablet of venlafaxine HCl using the combination of hydrophilic and hydrophobic polymers to prolong the effect with rate controlled drug release. Methods: The controlled release core in cup matrix tablets of venlafaxine HCl were prepared using HPMC K5, K4, K15, HCO, IPA, aerosol, magnesium sterate, hydrogenated castor oil and micro crystalline cellulose PVOK-900 using wet granulation technique. Total ten formulations with varying concentrations of polymers were prepared and evaluated for different physicochemical parameters such FTIR analysis for drug identification, In-vitro drug dissolution study was performed to evaluate the amount of drug release in 24 hrs, drug release kinetics study was performed to fit the data in zero order, first order, Hixson–crowell and Higuchi equation to determine the mechanism of drug release and stability studies for 3 months as observed. Results: The results of hardness, thickness, weight variation, friability and drug content study were in acceptable range for all formulations. Based on the In vitro dissolution profile, formulation F-9 was considered to be the optimized extending the release of 98.32% of drug up to 24 hrs. The data fitting study showed that the optimized formulation followed the zero order release rate kinetics and also compared with innovator product (flavix XR) showed better drug release profile. Conclusion: The core-in-cup technology has a potential to control the release rate of freely water soluble drugs for single administration per day by optimization with combined use of hydrophilic and hydrophobic polymers.

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Nanoformulation and Evaluation of Oral Berberine-Loaded Liposomes

Molecules ◽

10.3390/molecules26092591 ◽

2021 ◽

Vol 26 (9) ◽

pp. 2591

Author(s):

Thuan Thi Duong ◽

Antti Isomäki ◽

Urve Paaver ◽

Ivo Laidmäe ◽

Arvo Tõnisoo ◽

...

Keyword(s):

Thin Film ◽

Drug Release ◽

Size Distribution ◽

Water Soluble ◽

Release Behavior ◽

Uniform Size ◽

Ethanol Injection ◽

Drug Release Behavior ◽

Poorly Water Soluble

Berberine (BBR) is a poorly water-soluble quaternary isoquinoline alkaloid of plant origin with potential uses in the drug therapy of hypercholesterolemia. To tackle the limitations associated with the oral therapeutic use of BBR (such as a first-pass metabolism and poor absorption), BBR-loaded liposomes were fabricated by ethanol-injection and thin-film hydration methods. The size and size distribution, polydispersity index (PDI), solid-state properties, entrapment efficiency (EE) and in vitro drug release of liposomes were investigated. The BBR-loaded liposomes prepared by ethanol-injection and thin-film hydration methods presented an average liposome size ranging from 50 nm to 244 nm and from 111 nm to 449 nm, respectively. The PDI values for the liposomes were less than 0.3, suggesting a narrow size distribution. The EE of liposomes ranged from 56% to 92%. Poorly water-soluble BBR was found to accumulate in the bi-layered phospholipid membrane of the liposomes prepared by the thin-film hydration method. The BBR-loaded liposomes generated by both nanofabrication methods presented extended drug release behavior in vitro. In conclusion, both ethanol-injection and thin-film hydration nanofabrication methods are feasible for generating BBR-loaded oral liposomes with a uniform size, high EE and modified drug release behavior in vitro.

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The Correlation between Physical Crosslinking and Water-Soluble Drug Release from Chitosan-Based Microparticles

Pharmaceutics ◽

10.3390/pharmaceutics12050455 ◽

2020 ◽

Vol 12 (5) ◽

pp. 455

Author(s):

Emilia Szymańska ◽

Katarzyna Woś-Latosi ◽

Julia Jacyna ◽

Magdalena Dąbrowska ◽

Joanna Potaś ◽

...

Keyword(s):

Drug Release ◽

Polymer Matrix ◽

Drug Loading ◽

Water Soluble ◽

Dissolution Behavior ◽

Complex Nature ◽

Prolonged Release ◽

Scanning Calorimetry ◽

Burst Effect ◽

The Impact

Microparticles containing water-soluble zidovudine were prepared by spray-drying using chitosan glutamate and beta-glycerophosphate as an ion crosslinker (CF). The Box–Behnken design was applied to optimize the microparticles in terms of their drug loading and release behavior. Physicochemical studies were undertaken to support the results from dissolution tests and to evaluate the impact of the crosslinking ratio on the microparticles’ characteristics. The zidovudine dissolution behavior had a complex nature which comprised two phases: an initial burst effect followed with a prolonged release stage. The initial drug release, which can be modulated by the crosslinking degree, was primarily governed by the dissolution of the drug crystals located on the microparticles’ surfaces. In turn, the further dissolution stage was related to the drug diffusion from the swollen polymer matrix and was found to correlate with the drug loading. Differential Scanning Calorimetry (DSC) studies revealed the partial incorporation of a non-crystallized drug within the polymer matrix, which correlated with the amount of CF. Although CF influenced the swelling capacity of chitosan glutamate microparticles, surprisingly a higher amount of CF did not impact the time required for 80% of the drug to be released markedly. The formulation with the lowest polymer:CF ratio, 3:1, was selected as optimal, providing satisfactory drug loading and displaying a moderate burst effect within the first 30 min of the study, followed with a prolonged drug release of up to 210 min.

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