scholarly journals Formulation Development of a Food-Graded Curcumin-Loaded Medium Chain Triglycerides-Encapsulated Kappa Carrageenan (CUR-MCT-KC) Gel Bead Based Oral Delivery Formulation

Materials ◽  
2021 ◽  
Vol 14 (11) ◽  
pp. 2783
Author(s):  
Kei-Xian Tan ◽  
Ling-Ling Evelyn Ng ◽  
Say Chye Joachim Loo
Keyword(s):  
Delivery System ◽  
Oral Delivery ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Beta Carotene ◽  
Natural Polymers ◽  
Formulation Development ◽  
New Research ◽  
Kappa Carrageenan

In recent years, curcumin has been a major research endeavor in food and biopharmaceutical industries owing to its miscellaneous health benefits. There is an increasing amount of research ongoing in the development of an ideal curcumin delivery system to resolve its limitations and further enhance its solubility, bioavailability and bioactivity. The emergence of food-graded materials and natural polymers has elicited new research interests into enhanced pharmaceutical delivery due to their unique properties as delivery carriers. The current study is to develop a natural and food-graded drug carrier with food-derived MCT oil and a seaweed-extracted polymer called k-carrageenan for oral delivery of curcumin with improved solubility, high gastric resistance, and high encapsulation of curcumin. The application of k-carrageenan as a structuring agent that gelatinizes o/w emulsion is rarely reported and there is so far no MCT-KC system established for the delivery of hydrophobic/lipophilic molecules. This article reports the synthesis and a series of in vitro bio-physicochemical studies to examine the performance of CUR-MCT-KC as an oral delivery system. The solubility of CUR was increased significantly using MCT with a good encapsulation efficiency of 73.98 ± 1.57% and a loading capacity of 1.32 ± 0.03 mg CUR/mL MCT. CUR was successfully loaded in MCT-KC, which was confirmed using FTIR and SEM with good storage and thermal stability. Dissolution study indicated that the solubility of CUR was enhanced two-fold using heated MCT oil as compared to naked or unformulated CUR. In vitro release study revealed that encapsulated CUR was protected from premature burst under simulated gastric environment and released drastically in simulated intestinal condition. The CUR release was active at intestinal pH with the cumulative release of >90% CUR after 5 h incubation, which is the desired outcome for CUR absorption under human intestinal conditions. A similar release profile was also obtained when CUR was replaced with beta-carotene molecules. Hence, the reported findings demonstrate the potencies of MCT-KC as a promising delivery carrier for hydrophobic candidates such as CUR.

scholarly journals Development of Piperine-Loaded Solid Self-Nanoemulsifying Drug Delivery System: Optimization, In-Vitro, Ex-Vivo, and In-Vivo Evaluation

Nanomaterials ◽  
2021 ◽  
Vol 11 (11) ◽  
pp. 2920
Author(s):  
Ameeduzzafar Zafar ◽  
Syed Sarim Imam ◽  
Nabil K. Alruwaili ◽  
Omar Awad Alsaidan ◽  
Mohammed H. Elkomy ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Delivery ◽  
Ex Vivo ◽  
In Vitro Release ◽  
System Optimization ◽  
Globule Size

Hypertension is a cardiovascular disease that needs long-term medication. Oral delivery is the most common route for the administration of drugs. The present research is to develop piperine self-nanoemulsifying drug delivery system (PE-SNEDDS) using glyceryl monolinoleate (GML), poloxamer 188, and transcutol HP as oil, surfactant, and co-surfactant, respectively. The formulation was optimized by three-factor, three-level Box-Behnken design. PE-SNEDDs were characterized for globule size, emulsification time, stability, in-vitro release, and ex-vivo intestinal permeation study. The optimized PE-SNEDDS (OF3) showed the globule size of 70.34 ± 3.27 nm, percentage transmittance of 99.02 ± 2.02%, and emulsification time of 53 ± 2 s Finally, the formulation OF3 was transformed into solid PE-SNEDDS (S-PE-SNEDDS) using avicel PH-101 as adsorbent. The reconstituted SOF3 showed a globule size of 73.56 ± 3.54 nm, PDI of 0.35 ± 0.03, and zeta potential of −28.12 ± 2.54 mV. SEM image exhibited the PE-SNEDDS completely adsorbed on avicel. Thermal analysis showed the drug was solubilized in oil, surfactant, and co-surfactant. S-PE-SNEDDS formulation showed a more significant (p < 0.05) release (97.87 ± 4.89% in 1 h) than pure PE (27.87 ± 2.65% in 1 h). It also exhibited better antimicrobial activity against S. aureus and P. aeruginosa and antioxidant activity as compared to PE dispersion. The in vivo activity in rats exhibited better (p < 0.05) antihypertensive activity as well as 4.92-fold higher relative bioavailability than pure PE dispersion. Finally, from the results it can be concluded that S-PE-SNEDDS might be a better approach for the oral delivery to improve the absorption and therapeutic activity.

scholarly journals Formulation Development and Characterisation of Gemifloxacin Mesylate and Loteprednol Etabonate Ophthalmic Ocuserts

2020 ◽  
Vol 11 (2) ◽  
pp. 2549-2557
Author(s):  
Swati Mayur Keny ◽  
Ketan Shah
Keyword(s):  
Drug Release ◽  
Delivery System ◽  
In Vitro Release ◽  
Antibacterial Drug ◽  
Formulation Development ◽  
Loteprednol Etabonate ◽  
In Vitro Drug Release ◽  
Solvent Cast ◽  
Release Study

Gemifloxacin Mesylate is a fluoroquinolone antibacterial drug preferably used in the treatment of bacterial conjunctivitis. The addition of Loteprednol Etabonate enhances the anti-inflammatory activity of the developed formulation. The objective of the present work was to develop ocular inserts of Gemifloxacin Mesylate with Loteprednol Etabonate and thereby evaluate its potential as a sustained ocular delivery system. Poor bioavailability and poor therapeutic responses are associated with conventional ophthalmic solutions due to many pre-corneal constraints. These constrain trigger the researcher's mind to formulate a controlled and sustained drug delivery system. Ocular inserts based on the solvent cast technique were formulated and characterized by in vitro drug release studies using a flow-through apparatus that simulated the eye conditions. Compatibility of Gemifloxacin Mesylate, Loteprednol Etabonate, polymer, and excipients was checked based on preformulation studies. Different combinations of Gemifloxacin Mesylate, Loteprednol Etabonate, Carbopol 974, 98 981, PEG 400, and glycerine were formulated by the solvent cast method and evaluated. Clarity, smoothness, surface pH, drug content, and in-vitro drug release study were the various parameters evaluated on the formulated ocusert. Formula GLE 74 fulfilled the needs of all organoleptic parameters and also the in-vitro release study. Based on in vitro correlation stability studies, it was concluded that this ocular inserts formulation could be a promising controlled release formulation.

scholarly journals Preparation and Evaluation of Zafirlukast Compression Coated Tablets for Chronotherapeutic Drug Delivery

2021 ◽  
pp. 154-166
Author(s):  
M. S. Neeharika ◽  
B. Jeevana Jyothi
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Solid Dispersion ◽  
Chemical Interaction ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Natural Polymers ◽  
Compression Coating

The objective of the present study was to formulate and evaluate an oral, time-controlled drug delivery system of Zafirlukast. Zafirlukast belongs to BCS class II drugs as it has poor aqueous solubility and good permeability. Hence an attempt has been made to improve its aqueous solubility by solid dispersion technique so that its dissolution, bioavailability, and therapeutic effect can be optimized. The optimized solid dispersion was then formulated into a chronotherapeutic drug delivery system by compression coating technology. FT-IR study revealed that there was no chemical interaction between the drug and polymers used. Tablets were prepared by direct compression method using different super disintegrants and then followed by compression coating using natural polymers. Pre-compression and post-compression parameters complied with the Pharmacopoeia limit for the tablets. In vitro release studies were performed and the results indicated the formulation Z9F9 to be the optimized formulation.

scholarly journals Formulation Development and Evaluation of Itraconazole Loaded Invasomes Hydrogel

2021 ◽  
pp. 657-665
Author(s):  
Yogesh Singh ◽  
Anjana Bhardwaj
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Fungal Infections ◽  
In Vitro Release ◽  
The Body ◽  
Formulation Development ◽  
Drug Content ◽  
Carbopol 934P

Topical drug administration is a localized drug delivery system anywhere in the body through ophthalmic, rectal, vaginal and skin as topical routes. Skin is one of the most readily accessible organs on human body for topical administration and is main route of topical drug delivery system. There are various skin infections caused by fungus. An antifungal medication is a pharmaceutical fungicide used to treat mycoses such as athlete’s foot ringworm, candidiasis. Antifungal works by exploiting differences between mammalian and fungal cells to kill the fungal organism without dangerous effect on host. Itraconazole (ITZ) is commonly used in the treatment of fungal infections. It has low bioavailability (55%) because of low aqueous solubility and first pass effect. Hence we attempted to develop Itraconazole-loaded invasomes hydrogel. ITZ-loaded invasomes were prepared by conventional thin layer evaporation technique using Phospholipon 90H, terpene (Limonene) and ethanol. The optimized ITZ-loaded invasomes was incorporated into carbopol 934p (0.5 to 2%) solution to get a hydrogel for improving convenience in superficial application. FT-IR studies revealed no interaction between the drug and excipients. The formulated hydrogel formulation was evaluated with parameter pH, viscosity, gel strength, drug content, spread ability, in-vitro release test, wash ability, extrudability study and stability studies. The formulation OIGF4 showed a drug content of 99.12% and drug release of 99.78% in 72 hrs, which contains carbopol 934p concentration 2%w/w. The present work also focuses on making the formulation more pharmaceutically acceptable.

scholarly journals DRUG RELEASE CONTROL AND ENHANCEMENT USING CARRIERS WITH DIFFERENT CONCENTRATIONS OF CAPMUL® MCM C8

2021 ◽  
pp. 249-252
Author(s):  
MOHAMMAD F. BAYAN
Keyword(s):  
Drug Release ◽  
Oral Delivery ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Water Soluble ◽  
Swelling Behavior ◽  
Release Formulation ◽  
Poorly Soluble ◽  
Model Drug

Objective: The main aim of this study was to design a drug carrier capable to control and enhance the release of poorly water soluble drugs. Methods: Three polymeric formulations, based on poly (2-hydroxyethyl methacrylate) and loaded with different Capmul® MCM C8 concentrations (0, 10 and 20 % w/w), were prepared. Felodipine, which is a poorly soluble substance, was selected as a model drug. The effect of Capmul® MCM C8 on swelling behavior and in vitro release profile of the prepared polymer was investigated in PBS. Results: The swelling profiles of allformulationswere statistically similar, which indicated the non-significant effect of added Capmul® MCM C8 on polymer's swelling behavior. All formulations showed a delayed drug release. Formulation-F3, which is loaded with 20% w/wCapmul® MCM C8 displayed a significant higher release compared to the other formulations. Conclusion: Capmul® MCM products, which are widely used in food industries, can be used to improve the oral delivery of poorly soluble substances. The optimized formulation exhibited the ability to control and enhance the release of the model drug.

The in vitro release features of 5-Fluorouracil from tablets with chitosan, soy protein extract and chitosan-soyprotein extract blend as carriers and their thermal degradation characteristics

2021 ◽  
Vol 25 (7) ◽  
pp. 104-113
Author(s):  
K. Subramanian ◽  
G. Harivignesh ◽  
A. Jeevitha
Keyword(s):  
Drug Release ◽  
Thermal Degradation ◽  
Soy Protein ◽  
Food Packaging ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Natural Polymers ◽  
Protein Extract ◽  
Simulated Intestinal Fluid

Natural polymers are finding widespread applications in drug delivery, scaffold fabrication, bio plastic production, food packaging, wound dressing etc. due to their availability, biodegradability, biocompatibility, renewable nature, ease of modification to achieve the desirable properties etc. In the present study, the commercially available soy protein extract (SPE), chitosan(CSN) and their physical blend(CSN-SPE) have been chosen as drug carrier matrices to campare their in vitro drug release features in simulated intestinal fluid for controlled release applications taking 5-fluorouracil (5-FU) as a typical drug. The percentages of 5-FU released from the SPE, CSN and CSN-SPE tablets as a function of time were quantified by reverse phase High Performance Liquid Chromatography using KH2PO4 solution (pH 6.8) as the mobile phase and C-18 column as the stationery phase. The observed drug release features were found to be different for these polymer carriers. The percentages of drug released during the initial periods upto 60 min were less in the CSN-SPE tablet than those observed for CSN and SPE tablets. This implied that the drug release rate can be modified by the proper choice of natural polymers in the blends as carriers. The thermal degradation characteristics of CSN, SPE and CSN-SPE blend and their 5-FU tablets were also analysed by simultaneous Thermogravimetry (TG) and Differential Thermal Analysis (DTA). Comparative analysis of the TG and DTA traces of these polymers and their 5-FU tablets implied that there may be a drug-matrix interaction. This along with different degrees of swellability and degradability of these polymers might account for the differences in the drug release features. The structures of CSN, SPE and CSN-SPE blend were characterized by FT-IR spectroscopy.

scholarly journals Enhancement of Oral Bioavailability of Puerarin by Polybutylcyanoacrylate Nanoparticles

2011 ◽  
Vol 2011 ◽  
pp. 1-8 ◽  
Author(s):  
Lixia Zhao ◽  
Anchang Liu ◽  
Min Sun ◽  
Jinsong Gu ◽  
Haigang Wang ◽  
...  
Keyword(s):  
Zeta Potential ◽  
Oral Bioavailability ◽  
Oral Delivery ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Spherical Shape ◽  
Oral Drug ◽  
Burst Release ◽  
Vitro Release

The interest using novel drug delivery systems to improve oral bioavailability of drug with poor solubility is increasing. In this study, a new oral delivery system, polybutylcyanoacrylate nanoparticles (PBCNs), was introduced to improve the oral bioavailability of puerarin (PUE). PUE-loaded PBCN was successfully prepared by anionic polymerization method. Characterization of PUE-loaded PBCN was evaluated with morphology, size, zeta potential, and in vitro release study. The PBCN loading PUE exhibited a spherical shape under transmission electron microscopy with an average size of 159.4 nm, and the zeta potential was −15.0 mV. The in vitro release of PUE-loaded PBCN showed an initial burst release followed by a sustained release. Physicochemical state of PUE in PBCN was investigated by differential scanning colorimetry, X-ray diffraction, and Fourier transform infrared spectroscopy. The results indicated that PUE in PBCN was in a noncrystalline state. The oral pharmacokinetic study in rats showed that the relative bioavailability of PUE-encapsulated PBCN to the crude PUE was more than 550%. It can be concluded that PBCN as an oral drug carrier can significantly improve the oral bioavailability of PUE.

Fenofibrate Solid Dispersion for Improving Oral Bioavailability: Preparation, and Characterization and in vivo Evaluation

2020 ◽  
Vol 13 (5) ◽  
pp. 5102-5109
Author(s):  
Venu Madhav K ◽  
Somnath De ◽  
Chandra Shekar Bonagiri ◽  
Sridhar Babu Gummadi
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
In Vivo Evaluation

Fenofibrate (FN) is used in the treatment of hypercholesterolemia. It shows poor dissolution and poor oral bioavailability after oral administration due to high liphophilicity and low aqueous solubility. Hence, solid dispersions (SDs) of FN (FN-SDs) were develop that might enhance the dissolution and subsequently oral bioavailability. FN-SDs were prepared by solvent casting method using different carriers (PEG 4000, PEG 6000, β cyclodextrin and HP β cyclodextrin) in different proportions (0.25%, 0.5%, 0.75% and 1% w/v). FN-SDs were evaluated solubility, assay and in vitro release studies for the optimization of SD formulation. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) analysis was performed for crystalline and morphology analysis, respectively. Further, optimized FN-SD formulation evaluated for pharmacokinetic performance in Wistar rats, in vivo in comparison with FN suspension.  From the results, FN-SD3 and FN-SD6 have showed 102.9 ±1.3% and 105.5±3.1% drug release, respectively in 2 h. DSC and PXRD studies revealed that conversion of crystalline to amorphous nature of FN from FT-SD formulation. SEM studies revealed the change in the orientation of FN when incorporated in SDs. The oral bioavailability FN-SD3 and FN-SD6 formulations exhibited 2.5-folds and 3.1-folds improvement when compared to FN suspension as control. Overall, SD of FN could be considered as an alternative dosage form for the enhancement of oral delivery of poorly water-soluble FN.

Development, in vitro and in vivo Evaluations of Solid-Lipid Microparticles based on Solidified Micellar Carrier System for Oral Delivery of Cefepime

2017 ◽  
Vol 10 (1) ◽  
pp. 3582-3593
Author(s):  
Chukwuebuka Umeyor ◽  
Uchechukwu Nnadozie ◽  
Anthony Attama
Keyword(s):  
Oral Delivery ◽  
In Vitro Release ◽  
Carrier System ◽  
Solid Lipid ◽  
Solid Lipid Microparticles ◽  
Release Study ◽  
Lipid Microparticles ◽  
Vitro Release

This study seeks to formulate and evaluate a solid lipid nanoparticle-based, solidified micellar carrier system for oral delivery of cefepime. Cefepime has enjoyed a lot of therapeutic usage in the treatment of susceptible bacterial infections; however, its use is limited due to its administration as an injection only with poor patient compliance. Since oral drug administration encourage high patient compliance with resultant effect in improved therapy, cefepime was formulated as solid lipid microparticles for oral delivery using the concept of solidified micellar carrier system. The carrier system was evaluated based on particle yield, particle size and morphology, encapsulation efficiency (EE %), and thermal analysis using differential scanning calorimeter (DSC). Preliminary microbiological studies were done using gram positive and negative bacteria. In vitro release study was performed using biorelevant media, while in vivo release study was performed in white albino rats. The yield of solid lipid microparticles (SLM) ranged from 84.2 – 98.0 %. The SLM were spherical with size ranges of 3.8 ± 1.2 to 42.0 ± 1.4 µm. The EE % calculated ranged from 83.6 – 94.8 %. Thermal analysis showed that SLM was less crystalline with high potential for drug entrapment. Microbial studies showed that cefepime retained its broad spectrum anti-bacterial activity. In vitro release showed sustained release of cefepime from SLM, and in vivo release study showed high concentration of cefepime released in the plasma of study rats. The study showed that smart engineering of solidified micellar carrier system could be used to improve oral delivery of cefepime.

Formulation and Evaluation of Immediate Release Bilayer Tablets of Telmisartan and Hydrochlorothiazide

2011 ◽  
Vol 4 (3) ◽  
pp. 1477-1483
Author(s):  
Natarajan R ◽  
N Patel ◽  
Rajendran N N ◽  
M Rangapriya
Keyword(s):  
Antihypertensive Drugs ◽  
In Vitro Release ◽  
Immediate Release ◽  
Wet Granulation ◽  
Physical Parameters ◽  
Dissolution Profile ◽  
Formulation Development ◽  
Sodium Starch Glycolate ◽  
Bilayer Tablets

The main goal of this study was to develop a stable formulation of antihypertensive drugs telmisartan and hydrochlorothiazide as an immediate-release bilayer tablet and to evaluate the dissolution profile in comparison with a reference product. The formulation development work was initiated with wet granulation. Telmisartan was converted to its sodium salt by dissolving in aqueous solution of sodium hydroxide to improve solubility and drug release. Lactose monohydrate and microcrystalline cellulose were used as diluents. Starch paste is prepared in purified water and was used as the binder. Sodium starch glycolate is added as a disintegrating agent. Magnesium stearate was used as the lubricant. The prepared granules were compressed into a double-layer compression machine. The tablets thus formulated with higher proportion of sodium starch glycolate showed satisfactory physical parameters, and it was found to be stable and in vitro release studies are showed that formulation (F-T5H5) was 101.11% and 99.89% respectively. The formulation T5H5 is further selected and compared with the release profile of the innovator product, and was found to be similar (f2 factor) to that of the marketed product. The results suggest the feasibility of developing bilayer tablets consisting of telmisartan and hydrochlorothiazide for the convenience of patients with hypertension.  

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