scholarly journals Poloxamer 407-Based Thermosensitive Emulgel as a Novel Formulation Providing a Controlled Release of Oil-Soluble Pharmaceuticals—Ibuprofen Case Study

Materials ◽  
2021 ◽  
Vol 14 (23) ◽  
pp. 7266
Author(s):  
Kamil P. Grela ◽  
Dominik M. Marciniak ◽  
Bożena Karolewicz
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Castor Oil ◽  
Oil Content ◽  
Poloxamer 407 ◽  
Isopropyl Myristate ◽  
Cellulose Membrane ◽  
Oil In Water ◽  
Injection Force ◽  
Novel Drug

This article covers the design and evaluation of a novel drug vehicle: a thermosensitive, injectable, high-oil-content (50% w/w) emulgel providing a controlled release of lipophilic pharmaceuticals. Different vegetable (castor, canola, olive, peanut, grapeseed, linseed), mineral (paraffin) and semisynthetic (isopropyl myristate, oleic acid) oils were screened for ibuprofen (IBU) solubility and for their capacity for high-shear emulsification in a 17% (w/w) aqueous solution of poloxamer 407. Chosen emulgels were subject to a rheological evaluation, a syringeability test (TA.XT texture analyser; 2 mL syringe; 18 G, 20 G and 22 G needles) and a drug release study (48 h; cellulose membrane; 0.05 mol/L phosphate buffer at pH 7.4). Castor oil turned out to be an optimal component for IBU incorporation. Blank and drug-loaded castor oil emulgels were susceptible to administration via a syringe and needle, with the absolute injection force not exceeding 3 kg (29.4 N). The drug release test revealed dose-dependent, quasi-linear kinetics, with up to 44 h of controlled, steady, linear release. The results indicate the significant potential of high-oil-content, oil-in-water thermosensitive emulgel formulations as vehicles for the controlled release of lipophilic APIs.

Preparation of Liquid Oral Mucoadhesive Gastro-retentive System of Nimodipine

2019 ◽  
Vol 16 (9) ◽  
pp. 862-871 ◽  
Author(s):  
Mai Mamdouh ◽  
Ahmed Donia ◽  
Ebtessam Essa ◽  
Gamal El Maghraby
Keyword(s):  
Critical Care ◽  
Controlled Release ◽  
Drug Release ◽  
Release Rate ◽  
Poloxamer 407 ◽  
Liquid Form ◽  
Drug Release Rate ◽  
Alginate Concentration ◽  
Gastro Retentive

Background: Nimodipine is a calcium channel blocker frequently used in critical care settings. It is mainly absorbed in the upper gastrointestinal tract. Accordingly, the development of gastroretentive formulation will be beneficial. The benefit would be maximized for critical care patients if the developed system was in liquid form to facilitate the administration through nasogastric tubing. Objective: Development of gastro-retentive liquid oral controlled release formulation of nimodipine through in situ gellation. Methods: Nimodipine dissolution was improved by solid dispersion (SD) using poloxamer 407. Sodium alginate solutions (1, 1.5 and 2%w/v) were loaded with the optimized SD microparticles. Carboxymethylcellulose was added to modulate the release and to augment mucoadhesion power. All in situ gelling alginate solutions were characterized regarding viscosity, gelling capacity and drug release. SD microparticles showed considerable improvement in nimodipine dissolution. Results: All alginate systems were pourable. Increasing alginate concentration increased the gelling capacity and reduced drug release rate. The addition of carboxymethylcellulose produced greater control over drug release rate. X-ray radiography showed successful stomach-retention over 8 hours in rabbits, which correlates with the controlled release pattern of the developed systems. Conclusion: The study provides the formulator with a range of gastroretentive controlled release formulations of nimodipine while maintaining the convenience of administration through nasogastric tubing with the potential for enhanced bioavailability.

Evaluation of castorbean samples by economically - valuable traits

2018 ◽  
pp. 39-48
Keyword(s):  
Ricinoleic Acid ◽  
Castor Bean ◽  
Castor Oil ◽  
Oil Content ◽  
Climatic Conditions ◽  
Second Order ◽  
Yield Potential ◽  
Technological Parameters ◽  
Potential Yield ◽  
Ricinolic Acid

Castor oil (Ricinus communus L.) is an important commercial product. The climatic conditions of Ukraine determine the possibility of growing the castor as an annual crop. At the Institute of Oilseeds NAAS studied castor collection. The aim of the work was the selection of the most promising samples of castor oil, combining a large yield potential in a narrow range of vertical distribution for optimal technological parameters of mechanical harvesting with a high content of oil in seeds and ricinolic acid in oil. In the experience of 2015-2016, the manifestation of morphological features of 17 castor bean samples was studied. The height of plants, individual samples among themselves differed more than twice. Long-brush samples of ЕР118, К374, М203, К159 are distinguished on the basis of the length of the brush. The shortest brush was observed in sample K1008. The length of the productive brush in the studied samples is from 10.7 to 32.9 cm. Most castor bean samples under favorable conditions form brushes of the second and higher orders. According to this parameter, samples of Ep118 and selection No. 38 with four inflorescences of the second order are of the greatest interest. The largest brushes of the second order are similar in size to the brushes of the first order were observed in the samples: К1127, К810, К153. The adaptability of harvesting castor beads requires that the brushes of the first and second order coincide in height with each other, since the harvester can take a maximum of 60 cm. For the sum of the productive brushes of the first and second orders, the greatest potential yield will be provided by samples K159 and K1127. Among the studied collection stands out the small seed sample K159 and the large seed samples - PRL41 and K80. The average oil content in the seeds of the collection was from 52 to 61.4%. Sample38 had the highest oil content. The content of ricinolic acid in the collection was from 70.9 to 82.9%. Samples were isolated: К134, К1008, PRL41, К430 with the content of ricinoleic acid more than 80%. The results of the study of all parameters make it possible to isolate valuable technological samples. Sample K1064 with a high technological potential of productivity, with a seed oil content of 57.2%, has a not very high content of ricinoleic acid of 74.3%. Sample K1127 with an oil content of 58.6%, a mass of 1000 seeds of 265 g, a high potential of productive brushes has a wide variation in the arrangement of brushes. Sample K134 with a oil content of 57.1%, ricinoleic acid content of 80.7% has small second-order brushes and can be used as a single-cysts in a thicker seeding.

Development and Evaluation of Controlled Release Mucoadhesive Tablets of Captopril

1970 ◽  
Vol 9 (3) ◽  
pp. 3318-3329
Author(s):  
Kranthi Kumar Kotta ◽  
L. Srinivas
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Xanthan Gum ◽  
Diffusion Mechanism ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Content Uniformity ◽  
In Vitro Drug Release ◽  
Mucoadhesive Tablets

The present investigation focuses on the development of mucoadhesive tablets of captopril which are designed to prolong the gastric residence time after oral administration. Matrix tablets of captopril were formulated using four mucoadhesive polymers namely guar gum, xanthan gum, HPMC K4M and HPMC K15M and studied for parameters such as weight variation, thickness, hardness, content uniformity, swelling index, mucoadhesive force and in vitro drug release. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M provide slow release of captopril over period of 12 hr and were found suitable for maintenance portion of oral controlled release tablets. The cumulative % of drug release of formulation F9 and F10 were 90 and 92, respectively. In vitro release from these tablets was diffusion controlled and followed zero order kinetics. The ‘n’ values obtained from the pappas-karsemeyer equation suggested that all the formulation showed drug release by non-fickian diffusion mechanism. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M (1:1) were established to be the optimum formulation with optimum bioadhesive force, swelling index & desired invitro drug release. This product was further subjected to stability study, the results of which indicated no significant change with respect to Adhesive strength and in vitro drug release study.

Formulation and Evaluation of Nelfinavir Extended Release Trilayer Matrix Tablets by Design of Experiment

2018 ◽  
Vol 11 (5) ◽  
pp. 4259-4268
Author(s):  
Nirmala Rangu ◽  
Gande Suresh
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Magnesium Stearate ◽  
Zero Order ◽  
Matrix Tablets ◽  
Drug Dissolution ◽  
Crystalline Cellulose ◽  
Dissolution Profile ◽  
Release Formulation

The present study was aimed to develop once-daily controlled release trilayer matrix tablets of nelfinavir to achieve zero-order drug release for sustained plasma concentration. Nelfinavir trilayer matrix tablets were prepared by direct compression method and consisted of middle active layer with different grades of hydroxypropyl methylcellulose (HPMC), PVP (Polyvinyl Pyrrolidine) K-30 and MCC (Micro Crystalline Cellulose). Barrier layers were prepared with Polyox WSR-303, Xanthan gum, microcrystalline cellulose and magnesium stearate. Based on the evaluation parameters, drug dissolution profile and release drug kinetics DF8 were found to be optimized formulation. The developed drug delivery system provided prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (DF8) was described by the zero-order and best fitted to Higuchi model. FT-IR studies confirmed that there were no chemical interactions between drug and excipients used in the formulation. These results indicate that the approach used could lead to a successful development of a controlled release formulation of nelfinavir in the management of AIDS.

Optimization Study to Develop Once-a-day Controlled Release Formulation of Metoclopramide with Predictable Design Space

1970 ◽  
Vol 1 (1) ◽  
pp. 71-76
Author(s):  
Rajesh Dubey ◽  
Udaya K. Chowdary ◽  
Venkateswarlu V.
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Design Space ◽  
Release Kinetics ◽  
Release Profile ◽  
Release Formulation ◽  
Linear Effect ◽  
Controlled Release Formulation ◽  
The Difference ◽  
Face Centered

A controlled release formulation of metoclopramide was developed using a combination of hypromellose (HPMC) and hydrogenated castor oil (HCO). Developed formulations released the drug over 20 hr with release kinetics following Higuchi model. Compared to HCO, HPMC showed significantly higher influence in controlling the drug release at initial as well as later phase. The difference in the influence can be explained by the different swelling and erosion behaviour of the polymers. Effect of the polymers on release was optimized using a face-centered central composite design to generate a predictable design space. Statistical analysis of the drug release at various levels indicated a linear effect of the polymers’ levels on the drug release. The release profile of formulations containing the polymer levels at extremes of their ranges in design space was found to be similar to the predicted release profile

Nanoemulsions Loaded with Amphotericin B: Development, Characterization and Leishmanicidal Activity

2019 ◽  
Vol 25 (14) ◽  
pp. 1616-1622 ◽  
Author(s):  
Gabriela Muniz Félix Araújo ◽  
Gabriela Muniz Félix Araújo ◽  
Alana Rafaela Albuquerque Barros ◽  
Alana Rafaela Albuquerque Barros ◽  
João Augusto Oshiro-Junior ◽  
...  
Keyword(s):  
Amphotericin B ◽  
Average Diameter ◽  
Isopropyl Myristate ◽  
Neglected Diseases ◽  
Clinical Form ◽  
Hydrophobic Compounds ◽  
Internal Phase ◽  
Oil In Water ◽  
Spherical Structures ◽  
Lipid Formulations

Leishmaniasis is one of the most neglected diseases in the world. Its most severe clinical form, called visceral, if left untreated, can be fatal. Conventional therapy is based on the use of pentavalent antimonials and includes amphotericin B (AmB) as a second-choice drug. The micellar formulation of AmB, although effective, is associated with acute and chronic toxicity. Commercially-available lipid formulations emerged to overcome such drawbacks, but their high cost limits their widespread use. Drug delivery systems such as nanoemulsions (NE) have proven ability to solubilize hydrophobic compounds, improve absorption and bioavailability, increase efficacy and reduce toxicity of encapsulated drugs. NE become even more attractive because they are inexpensive and easy to prepare. The aim of this work was to incorporate AmB in NE prepared by sonicating a mixture of surfactants, Kolliphor® HS15 (KHS15) and Brij® 52, and an oil, isopropyl myristate. NE exhibited neutral pH, conductivity values consistent with oil in water systems, spherical structures with negative Zeta potential value, monomodal size distribution and average diameter of drug-containing droplets ranging from 33 to 132 nm. AmB did not modify the thermal behavior of the system, likely due to its dispersion in the internal phase. Statistically similar antileishmanial activity of AmB-loaded NE to that of AmB micellar formulation suggests further exploring them in terms of toxicity and effectiveness against amastigotes, with the aim of offering an alternative to treat visceral leishmaniasis.

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

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.

Porous SBA-15/cellulose membrane with prolonged anti-microbial drug release characteristics for potential wound dressing application

Cellulose ◽  
2020 ◽  
Vol 27 (5) ◽  
pp. 2737-2756
Author(s):  
Zhi Shen ◽  
Ning Cai ◽  
Yanan Xue ◽  
Bo Yu ◽  
Jianzhi Wang ◽  
...  
Keyword(s):  
Drug Release ◽  
Wound Dressing ◽  
Cellulose Membrane

scholarly journals Drug release from thin films encapsulated by a temperature-responsive hydrogel

Soft Matter ◽  
2019 ◽  
Vol 15 (8) ◽  
pp. 1853-1859 ◽  
Author(s):  
Oliver Werzer ◽  
Stephan Tumphart ◽  
Roman Keimel ◽  
Paul Christian ◽  
Anna Maria Coclite
Keyword(s):  
Thin Films ◽  
Controlled Release ◽  
Drug Release ◽  
Temperature Responsive ◽  
Temperature Controlled ◽  
Drug Polymer Interaction ◽  
Polymer Interaction

Temperature-controlled release and study on the effects of the drug–polymer interaction and pH.

Pectin-Chitosan Multilayer Coated Microbeads of Diclofenac Sodium Prepared by Layer-by-Layer Technique

2014 ◽  
Vol 1060 ◽  
pp. 45-49
Author(s):  
Kamonrak Cheewatanakornkool ◽  
Pornsak Sriamornsak
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Diclofenac Sodium ◽  
Gastric Fluid ◽  
Layer By Layer ◽  
Release Behavior ◽  
Freeze Dried ◽  
Layer Technique ◽  
Calcium Pectinate ◽  
Layer By Layer Technique

The main objective of this study was to fabricate biopolymer-based microbeads, providing enteric properties and controlled release of diclofenac sodium, using layer-by-layer technique. The calcium pectinate microbeads have been designed and coated with chitosan and pectin multilayers. Drug release was performed in simulate gastric fluid (pH 1.2) for 2 hours, followed by pH 6.8 buffer for 8 hours. The effects of chitosan concentration, number of layer and drying technique on drug release were investigated. The results showed that the calcium pectinate microbeads could be simply prepared by ionotropic gelation and then coated with chitosan and pectin solutions using layer-by-layer procedure. The diameter of the microbeads ranged from 800 to 1000 μm for air-dried samples and from 1 to 2 mm for freeze-dried samples. The freeze-dried microbeads had a rough surface and many pores inside, as observed by SEM. The microbeads coated with 4% chitosan/4% pectin revealed a slower drug release than those coated with 1% chitosan/4% pectin and demonstrated a controlled release pattern. Moreover, different drying techniques and numbers of layer also influenced drug release behavior of the prepared microbeads.

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