scholarly journals Mechanically Robust Gastroretentive Drug-Delivery Systems Capable of Controlling Dissolution Behaviors of Coground β-Lapachone

Pharmaceutics ◽  
2019 ◽  
Vol 11 (6) ◽  
pp. 271 ◽  
Author(s):  
Hyeongmin Kim ◽  
Chung-Lyol Lee ◽  
Seohyun Lee ◽  
Tae Jin Lee ◽  
Iqra Haleem ◽  
...  
Keyword(s):  
Mechanical Properties ◽  
Drug Delivery ◽  
Amorphous State ◽  
Aqueous Solubility ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Dissolution Behavior ◽  
Matrix Tablet ◽  
Freeze Thaw ◽  
Physically Crosslinked

In this study, we aimed to design a highly swellable and mechanically robust matrix tablet (SMT) as a gastroretentive drug-delivery system (GRDDS) capable of improving the dissolution behavior of β-lapachone with low aqueous solubility. For the preparation of SMTs, the cogrinding technique and freeze–thaw method were used to disperse β-lapachone in SMTs in an amorphous state and to enhance the swelling and mechanical properties of SMTs, respectively. As a result, the crystallinity of coground β-lapachone incorporated in the SMTs was found to be considerably decreased; thereby, the dissolution rates of the drug in a simulated gastric fluid could be substantially increased. The SMTs of β-lapachone also demonstrated significantly enhanced swelling and mechanical properties compared to those of a marketed product. The reason for this might be because the physically crosslinked polymeric networks with a porous structure that were formed in SMTs through the freeze–thaw method. In addition, β-lapachone was gradually released from the SMTs in 6 h. Therefore, SMTs of β-lapachone developed in this study could be used as GRDDS with appropriate swelling and mechanical properties for improving the dissolution behavior of hydrophobic drugs such as β-lapachone.

Role of Biorelevant Media in Estimation of in vitro Lipolysis and Food Impact on Self-emulsifying Drug Delivery Systems.

2020 ◽  
Vol 15 ◽  
Author(s):  
Ravinder Verma ◽  
Deepak Kaushik
Keyword(s):  
Drug Delivery ◽  
Small Intestine ◽  
Drug Delivery Systems ◽  
Food Effect ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Biorelevant Media ◽  
In Vitro Lipolysis ◽  
Fasted State

: Self-emulsifying drug delivery systems (SEDDS) includes self-micro emulsifying drug delivery system (SMEDDS) and self-nano emulsifying drug delivery system (SNEDDS) whose major benefits is reduction of inter/intra subject variability and food effect which may alter the pharmacological response of the drug. Oral intake of these formulations triggers the digestion process because of pancreatic lipase which emulsify/digest the lipidic ingredients of the formulation resulting into precipitation of the drug. As a tool to foresee in vivo medicament precipitation, in vitro lipolysis models are established. Biorelevant media play an important role to study the effect of in vitro lipolysis and food impact on the bioavailability of SEDDS formulations. It is vital to generate composition of fluids for both fed and fasting conditions of gastric, small intestine and colon to investigate the impact of in vitro lipolysis and food effect on the release behavior of drug from SEDDS. Fed/Fasted state simulated gastric fluid (Fe/FaSSGF), Fed/Fasted state simulated gastric fluid (Fe/FaSSIF) (Phosphate buffers) are first generation while Fa/FeSSIF-V2 (maleate) are second generation biorelevant media utilized for these studies. FaSSIF-V3 belongs to third generation which differs from other generations in the composition and source of bile salts. With updates in physiological data, it is vital to incorporate changes in the dissolution media to make it more biorelevant. This review paper mainly laid emphasis on the compositions of biorelevant media of gastric and small intestine for both fed and fasting conditions. In addition to these, applications of biorelevant to investigate effect of in vitro lipolysis and food on SEDDS are discussed with some recent research reports.

Preparation of Eudragit® L Beads for Intragastric Floating Drug Delivery

2014 ◽  
Vol 1060 ◽  
pp. 79-82 ◽  
Author(s):  
Tassanee Nernplod ◽  
Prasert Akkaramongkolporn ◽  
Pornsak Sriamornsak
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Gastric Fluid ◽  
Cetyl Alcohol ◽  
Simulated Gastric Fluid ◽  
Release Behavior ◽  
Slight Effect ◽  
Drug Release Behavior ◽  
Floating Drug Delivery ◽  
Enteric Polymer

The aim of this study was to prepare matrix beads made of enteric polymer, Eudragit® L, metronidazole and various amounts of cetyl alcohol (0, 0.1 and 1%). Eudragit® L, metronidazole and cetyl alcohol were dissolved in acetone and then extruded into dichloromethane. The influence of amount of cetyl alcohol on floating and drug release behavior of matrix beads of Eudragit® L was investigated. The results showed that, after extruding, cetyl alcohol dissolved out from the beads already formed, resulting in a porous structure. Thus, the beads can float in simulated gastric fluid for more than 8 hours. Different amounts of cetyl alcohol had a slight effect on the drug release. However, the increased amount of cetyl alcohol in the formulations significantly sustained the drug release while the beads remained floating. The results suggest that Eudragit® L beads could be used as a carrier for intragastric floating drug delivery.

Foldable/Expandable Gastro-retentive Films Based on Starch and Chitosan as a Carrier For Prolonged Release of Resveratrol

2021 ◽  
Vol 22 ◽  
Author(s):  
Rattakorn Boontawee ◽  
Ousanee Issarachot ◽  
Kanidta Keawkroek ◽  
Ruedeekorn Wiwattanapatapee
Keyword(s):  
Corn Starch ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Prolonged Release ◽  
Therapeutic Effects ◽  
Natural Polymers ◽  
Gastric Diseases ◽  
Anti Inflammatory

Background: Resveratrol exerts a number of therapeutic effects, notably anti-inflammatory, antioxidant and anti-cancer activities which are beneficial for the treatment of gastric diseases. However, the efficacy of resveratrol is severely limited due to the poor aqueous solubility and rapid metabolism following oral administration. As a result, foldable/expandable devices based on natural polymers merging with solid dispersion technology have been developed to increase the solubility, prolong the gastric residence time, and provide a controlled release therapy of resveratrol. Objectives: This research aimed to invent foldable/expandable films based on natural polymers, including starch and chitosan, for stomach-specific delivery and prolonged release of resveratrol. Methods: The films were prepared by solvent casting using either rice, tapioca, corn starch or pre-gelatinized corn starch combined with chitosan in different weight to weight ratios. Glycerol was included as a plasticizer. Resveratrol solid dispersions (Res-SD) prepared by solvent evaporation and employing PVP-K30 as a hydrophilic polymer were loaded into the polymeric film, which was subsequently folded prior to insertion in a hard gelatin capsule. Results: The solid dispersions improved the solubility of resveratrol by a factor of 500. All Res-SD loaded film formulations completely unfolded in simulated gastric fluid at 37oC within 10 min. Fluid absorption by the films was influenced by the ratio of amylose and amylopectin in the starch granules, with tapioca starch formulations displaying the highest fluid uptake. Films prepared from pre-gelatinized corn starch and chitosan resulted in highly efficient delivery of resveratrol, with more than 80%of the content released over a period of 12 hrs. Furthermore, the released polyphenol exhibited cytotoxic activity against human gastric adenocarcinoma cells and anti-inflammatory effects against lipopolysaccharide-stimulated murine, macrophage-like cells. Conclusions: These findings demonstrate the potential of foldable/expandable films based on natural polymers as a promising stomach-specific carrier for improving the treatment of gastric disorders.

scholarly journals Interpolymer Complexes of Eudragit® Copolymers as Novel Carriers for Colon-Specific Drug Delivery

Polymers ◽  
2020 ◽  
Vol 12 (7) ◽  
pp. 1459
Author(s):  
Aleksandra V. Bukhovets ◽  
Nikoletta Fotaki ◽  
Vitaliy V. Khutoryanskiy ◽  
Rouslan I. Moustafine
Keyword(s):  
Drug Delivery ◽  
Photoelectron Spectroscopy ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Biorelevant Media ◽  
Simulated Intestinal Fluid ◽  
Swelling Properties ◽  
Interpolymer Complexes ◽  
Fasted State ◽  
The Media

Interpolymer complexes (IPC) based on Eudragit® EPO and Eudragit® S100 were investigated as potential carriers for oral controlled drug delivery to the colon. IPC samples were prepared by mixing copolymer solutions in organic solvents (ethanol, isopropanol:acetone mixture (60:40, % v/v) and tetrahydrofuran). According to the data of elemental analysis, FTIR-spectroscopy, X-ray photoelectron spectroscopy and thermal analysis these IPCs have excess of anionic copolymer (Eudragit® S100) in their structure; they are stabilized by hydrogen and ionic intermacromolecular bonds and do not include free copolymer domains. IPC have pH-independent swelling properties in the media mimicking gastrointestinal tract (GIT) conditions and provide colon-specific delivery of indomethacin in buffer solutions (pH 1.2; 5.8; 6.8; 7.4) and in biorelevant media (fasted state simulated gastric fluid, fasted state simulated intestinal fluid—version 2 and fasted stated simulated colonic fluid).

scholarly journals Physico-chemical evaluation of Gastroretentive Ranitidine Hydrochloride: An Anti-Ulcer Drug

2016 ◽  
Vol 3 (2) ◽  
pp. 4-12
Author(s):  
RK Yadav ◽  
Satyam Prakash ◽  
K Yadav ◽  
NK Yadav ◽  
M Mostafa
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Entrapment Efficiency ◽  
Lag Time ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Drug Content ◽  
Drug Entrapment Efficiency ◽  
Gastro Retentive

Background  and  Objectives:  The  prevention  and  treatment  of  peptic  ulcers  has  become  an important challenge in the current medicine  world.   Modern progress in novel drug delivery system aims to improve the efficacy of the drug molecule by formulating a dosage form of RHCL. One of the most feasible approaches for achieving a prolonged and predictable drug delivery profile in GI tract is to control the gastric residence time.  Therefore, a multi-unit gastro retentive dosage form of RHCL capable of floating on simulated gastric fluid for more than 12 hours was formulated and evaluated.Materials  and  Methods:  Nine  batches  of  the  light  liquid  paraffin  entrapped  emulsion  gel  beads were  prepared  by  a  new  emulsion  gelation  technique  using  sodium  alginate  and  xanthan  gum  as polymers.  The  polymeric  solution  was  extruded  into  Calcium  chloride  solution  by  the  use  of  21G needles.  Morphology  of  beads,  drug  content,  drug  entrapment  efficiency,  floating  lag  time  and buoyancy were studied. Compatibility study of Ranitidine HCl with polymers used in the formulation was performed using DSC and FT-IR.Results:  Mean  surface  diameter  were  between  1.220  ±  2.259%  (F1)  to  1.230  ±  2.316%  (F9)  and floating lag time were between 6 minute (F9) to 11 minute (F1). All formulations were buoyant for more than 12 hours in simulated gastric  fluid  at  37ºC.  The  drug  content  and  drug  entrapment efficiency  among  the  formulations  were  between  17.48%~19.68%  and  71.06%  ~84.32% respectively. Formulation F1 showed lowest drug content and drug entrapment efficiency while F9 showed highest drug content and drug entrapment efficiency. F4 showed most acceptable sustained drug release profile.Conclusion:  The gastro retentive drug delivery system designed as floating beads was found to be satisfactory drug delivery system for Ranitidine HCl to improve the bioavailability of the drug. Janaki Medical College Journal of Medical Sciences (2015) Vol. 3 (2): 4-12

Floating Alginate Beads as Carriers for Self-Emulsifying System Containing Tetrahydrocurcumin

2012 ◽  
Vol 506 ◽  
pp. 517-520 ◽  
Author(s):  
S. Sriraksa ◽  
N. Sermkaew ◽  
S. Setthacheewakul ◽  
R. Wiwattanapatapee
Keyword(s):  
Oral Delivery ◽  
Aqueous Suspension ◽  
Aqueous Solubility ◽  
Gastric Fluid ◽  
Alginate Beads ◽  
Water Soluble ◽  
Simulated Gastric Fluid ◽  
Pore Former ◽  
Gastric Residence Time

Tetrahydrocurcumin (THC), one of the curcumin metabolites, exhibits pharmacological activities such as antioxidant, anti-inflammatory and anti-carcinogenic properties. However, the pharmacological effect of THC is limited due to its low aqueous solubility. Floating alginate beads containing self-emulsifying drug delivery system (SEDDS) of THC were developed to increase drug solubility and prolong gastric residence time. Use of different weight proportions of sodium alginate (Na-alg.), calcium chloride (CaCl2) and water soluble pore former (Polyvinylalcohol-polyethylene glycol copolymer; Kollicoat® IR) in bead formulations had different effects on the floating abilities and in vitro rate of THC release. The release profile of the optimized THC-SEDDS floating alginate beads (D3) indicated a significant increase in the dissolution rate of THC and provided a controlled release of THC over an 8 h period in a simulated gastric fluid. The release of about 80% of THC from the optimized beads as an o/w microemulsion with a particle size of less than 50 nm, compared to only 30 % by an aqueous suspension from the unformulated THC could be considerable greater absorbed. The self-emulsifying floating alginate beads may provide a useful solid dosage form for oral delivery of THC and other hydrophobic compounds.

Design of cellulose derivative and alginate based smart polymers to develop stomach specific floating drug delivery system

2020 ◽  
Vol 05 ◽  
Author(s):  
Vikrant Sharma ◽  
Jogindera Devi
Keyword(s):  
Drug Delivery ◽  
Drug Loading ◽  
Diffusion Mechanism ◽  
Gastric Fluid ◽  
Fickian Diffusion ◽  
Simulated Gastric Fluid ◽  
Smart Polymers ◽  
Bead Size ◽  
Optimal Drug ◽  
Gastro Retentive

Background: Polysaccharide based gastro-retentive drug delivery systems (GRDDSs) can retain in the gastric fluid of stomach for longer time and release entrapped drug in controlled and localized manner, which can ensure optimal drug concentration at the site of action with improved bioavailability and reduced side effects of acid suppressive drugs like ranitidine. Objective: The objective of present study was to design smart polymers for gastro-retentive drug delivery of ranitidine through ionic-gelation of carboxymethyl cellulose (CMC) and sodium alginate (ALG). Methods: The optimal reaction conditions for synthesis of beads were evaluated by varying reaction parameters during synthesis and were obtained as [CMC] = 1.5% (w/v), [ALG] = 0.5% (w/v) and [CaCl2] = 0.1 M with maximum equilibrium swelling ratio (2922.50±0.90)%. The drug loading was carried out by simultaneous and swelling equilibrium methods. Beads were characterized by SEM, PXRD, FTIR, TGA, bead size and swelling studies. Results: Increase in Ca2+ ions and ALG concentration resulted in decrease in swelling capacity and increase in bead size. Beads got collapsed in phosphate buffer solution and swelling had been occurred through non-Fickian diffusion mechanism. Floating beads with (51.05±0.25)% entrapment efficiency for simultaneous drug loading method exhibited Fickian diffusion mechanism and best fitted in Higuchi model. The diffusion coefficient and initial rate of drug release in simulated gastric fluid demonstrated swelling controlled gastro-retentive release of ranitidine. Conclusion: These smart polymeric beads have potential to use as a promising candidate for the design of GRDDSs meant for the treatment of gastric ulceration and gastro-oesophageal reflux disease.

scholarly journals Synthesis and Characterization of Thiolated Gum Ghatti as a Novel Excipient: Development of Compression Coated Mu-Coadhesive Tablets of Domperidone

2021 ◽  
Author(s):  
Vivek Puri ◽  
Ameya Sharma ◽  
Pradeep Kumar ◽  
Inderbir Singh ◽  
Kampanart Huanbutta
Keyword(s):  
Drug Delivery ◽  
Oral Drug Delivery ◽  
Ex Vivo ◽  
Gastric Fluid ◽  
Hydroxyl Group ◽  
Simulated Gastric Fluid ◽  
Oral Drug ◽  
Ester Formation ◽  
In Silico Studies ◽  
Gum Ghatti

Background: Mucoadhesive polymers represent a major part of site-specific and localized retention strategies in oral drug delivery. Present research was designed to synthesize and characterize a novel mucoadhesive carbohydrate polymer (thiolated gum ghatti; TGG) which was further employed to fabricate mucoadhesive tablets of domperidone using an industrially viable compression coating technique. Methods: Thiolation of gum ghatti was achieved by the ester formation (esterification) between hydroxyl group and carboxyl group of gum ghatti and thioglycolic acid. Results: TGG was characterized by various physico-chemical techniques such as FTIR, XRD, SEM and DSC techniques. In rheological studies, the observed viscosities of pure gum-mucin were 45.45 and 71.75 mPas and that of thiolated gum were 78.7 and 112.58 mPas respectively in water and simulated gastric fluid. Signifi-cant increase in viscosity for thiolated gum may be attributed to increased macromolecular interactions responsible for enhanced mucoadhesive potential of thiolated gum. In-silico studies corroborate the role of mucin gum interaction and energetic stabilization for en-hanced mucoadhesion properties of thiolated gum. Ex-vivo mucoadhesion strength of gum ghatti and thiolated gum ghatti coated tablets was found to be ranging between 4.67± 0.79 to 8.99± 0.75 g and 11.76± 1.34 to 18.83± 2.07 g respectively. Conclusion: Thiolated gum ghatti may be regarded as a promising polymer for developing different mucoadhesive drug delivery systems.

Validation of A Simple HPLC-UV Method For the Quantification of Andrographolide in Self-Nano Emulsifying Drug Delivery System (Snedds) For Dissolution Study

2017 ◽  
Vol 7 (04) ◽  
Author(s):  
Syukri Y ◽  
Afetma D. W. ◽  
Sirin M. ◽  
Fajri R. ◽  
Ningrum A. D. K. ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Gastric Fluid ◽  
Hplc Method ◽  
Good Precision ◽  
Intestinal Fluid ◽  
Dissolution Medium ◽  
Relative Standard ◽  
Sufficient Precision

This research aim to validation of a simple, rapid and accurate HPLC-UV method for the quantification of andrographolide isolated from Andrographis paniculata Ness in Self Nano Emulsifying Drug Delivery System (SNEDDS) formulation during the dissolution test. The assay was performed using a XTerra® MS C18 column (150 mm X 4.6 mm, five μm) with a mobile phase of methanol and water (70: 30), at 0.8 mL/min flow rate and UV detection of 229 nm. Simulation gastric fluid (SGF) and intestinal fluid (SIF) were prepared as dissolution medium. The validation parameter was conducted including the test on linearity, precision, accuracy, LOD, and LOQ. The result showed an excellent linearity with r = 0.999 and good selectivity for both medium dissolution. The method showed sufficient precision, with a relative standard deviation (RSD) smaller than % Horwitz. The accuracy reported as % recovery was found to be 102.61 and 101.17 % in each SGF and SIF dissolution medium. LOD and LOQ were found 0.46 and 1.40 in SGF medium, 0.87 and 2.64 in SIF medium. In conclusion, the HPLC method developed showed specificity and selectivity with linearity in the working range, good precision and accuracy and suitable for quantification andrographolide in SNEDDS formulation.

A Review on Emerging Floating Drug Delivery System

2016 ◽  
Vol 6 (4) ◽  
Author(s):  
Christe Mary M ◽  
Sasikumar Swamiappan
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Stomach Contents ◽  
Gastric Fluid ◽  
Dosage Forms ◽  
Gastric Residence Time ◽  
Advantages And Disadvantages ◽  
Floating Drug Delivery ◽  
Floating Drug Delivery System

Presently, various approaches have been exploited in the prolongation of gastric residence time which includes floating drug delivery system (FDDS), swelling and expanding systems, bio-adhesive systems, modified shape systems and high density systems. Among various methods, floating drug delivery system is considered to be a predominant method. Gastric emptying of dosage forms is an extremely varying process and ability to extend and control the emptying time is a valuable resource for the dosage forms. This FDDS is having the ability to provides a solution for this purpose. The FDDS is a bulk density system lower than the gastric fluid, so that the rest will float on the stomach contents for a prolonged period of time and allowing the drug to release slowly at a desired rate from the system and intensifies the bio-availability of the drug having narrow absorption window. The main intension of writing this review on floating drug delivery system is to study the mechanism of flotation to acheive the gastric retention and to discuss briefly about the background of FDDS, advantages and disadvantages, application of FDDS and factors affecting the gastric retension time.

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