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 FLOATING-BIOADHESIVE MATRIX TABLETS OF HYDRALAZINE HCL MADE OF CASHEW GUM AND HPMC K4M

2017 ◽  
Vol 9 (7) ◽  
pp. 124 ◽  
Author(s):  
M. Saquib Hasnain ◽  
Poonam Rishishwar ◽  
Sadath Ali
Keyword(s):  
Ex Vivo ◽  
Diffusion Mechanism ◽  
Hydroxypropyl Methylcellulose ◽  
Gastric Fluid ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Simulated Gastric Fluid ◽  
Cashew Gum ◽  
Gastro Retentive

Objective: The objective of this paper was to prepare and evaluate floating-bioadhesive cashew gum-hydroxypropyl methylcellulose (HPMC K4M) matrix tablets for the gastro-retentive release of hydralazine HCl.Methods: The cashew gum-HPMC K4M matrix tablets of hydralazine HCl were prepared by direct compression method with the incorporation of sodium bicarbonate and citric acid as effervescent agents. Drug contents, weight variations, hardness, friability, in vitro swelling, in vitro floatation, ex vivo mucoadhesion and in vitro drug release of these matrix tablets were evaluated.Results: Drug contents, weight variations, hardness and friability of these matrix tablets were within the compendia limits. These tablets were floated well in vitro over 12 h in simulated gastric fluid (SGF, pH 1.2) with minimum lag time. The ex vivo adhesion of these matrix tablets with goat intestinal mucosa exhibited good bioadhesion in a wash off test. All these cashew gum-HPMC K4M floating-bioadhesive matrix tablets of hydralazine HCl showed in vitro sustained releases of hydralazine HCl over 12 h in SGF, pH 1.2. The in vitro hydralazine HCl followed Korsmeyer-Peppas kinetic model and anomalous (non-Fickian) diffusion mechanism. The drug-polymer compatibility analysis by FTIR spectroscopy indicated the absence of any drug-polymer interaction within this cashew gum-HPMC K4M floating-bioadhesive matrix tablets of hydralazine HCl.Conclusion: The results clearly indicate a promising potential of the use of cashew gum as matrix forming a material with HPMC K4M to prepare matrix tablets for gastro retentive delivery of hydralazine HCl through the combined approach of floatation and bioadhesion to reduce the dosing rate with better patient compliances.

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

Nanostructured Lipid Carriers (NLCs) for drug delivery: Role of Liquid lipid (oil)

2020 ◽  
Vol 17 ◽  
Author(s):  
Anisha D’Souza ◽  
Ranjita Shegokar
Keyword(s):  
Drug Delivery ◽  
Essential Oils ◽  
Drug Carrier ◽  
Drug Loading ◽  
Performance Criteria ◽  
Long Term Stability ◽  
Natural Oils ◽  
Optimal Drug

: In recent years, SLNs and NLCs are among the popular drug delivery systems studied for delivery of lipophilic drugs. Both systems have demonstrated several beneficial properties as an ideal drug-carrier, optimal drug-loading and good long-term stability. NLCs are getting popular due to their stability advantages and possibility to load various oil components either as an active or as a matrix. This review screens types of oils used till date in combination with solid lipid to form NLCs. These oils are broadly classified in two categories: Natural oils and Essential oils. NLCs offer range advantages in drug delivery due to the formation of imperfect matrix owing to the presence of oil. The type and percentage of oil used determines optimal drug loading and stability. Literature shows that variety of oils is used in NLCs mainly as matrix, which is from natural origin, triglycerides class. On the other hand, essential oils not only serve as a matrix but as an active. In short, oil is the key ingredient in formation of NLCs, hence needs to be selected wisely as per the performance criteria expected.

Fusion as an Approach to Enhance Dissolution Rate of a Poorly Water-Soluble Drug (Curcurmin)

2011 ◽  
Vol 393-395 ◽  
pp. 119-122
Author(s):  
Dong Hua Wan ◽  
Fen Lin ◽  
Qu Xiang Liao
Keyword(s):  
Dissolution Rate ◽  
Drug Loading ◽  
Solid Dispersions ◽  
Gastric Fluid ◽  
Molecular State ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Simulated Gastric Fluid ◽  
Scanning Calorimetry ◽  
Rate Improvement

It’s well known that curcumin is practically insoluble in water. Therefore, to improve the drug dissolution rate, fusion approach was employed to prepare curcumin solid dispersions (SDs) in the carrier Pluronic F68 with three different drug loads. The dissolution rate of curcumin from the SDs was measured at simulated gastric fluid. The concentration of the dissolved drug in the medium was determined by HPLC. The dissolution rates of the formulations were dependent on the drug loading in SDs. 92.2% CUR was dissolved in 10 min from the SDs with 8.97% drug load, whereas the amounts of drug released were 65.8% and 84.2% within 120 min from the SDs with 18.9% and 29.0% drug loads, respectively. The Fourier transform infrared spectra indicated hydrogen bond between the drug and carrier. Furthermore, their physicochemical properties were well investigated using differential scanning calorimetry and X-ray diffraction. In the dispersions containing 8.97% CUR, the drug was in the molecular state. At a composition of approximately 18.9%, CUR was dispersed as micro-fine crystals. These interesting results indicate that the physical states of the drug in the carrier, which are governed by the drug loading, can affect the dissolution rate improvement.

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.

scholarly journals Microballoons: A Gastro Retentive Drug Delivery System

2019 ◽  
Vol 9 (4-s) ◽  
pp. 625-630
Author(s):  
Ankita Srivastava ◽  
Ruchi Shukla ◽  
Kusum Sharma ◽  
Hitesh Jain ◽  
D. B. Meshram
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Gastric Fluid ◽  
Oral Route ◽  
Gastric Retention ◽  
Preparation Temperature ◽  
Novel Technology ◽  
Floating Drug Delivery ◽  
Gastro Retentive

Oral route is most preferable and widely used route for the administration of drug. Microballoons becomes novel technology in pharmaceutical field in the floating drug delivery for achieving the gastric retention. Microballoons are also called as hollowspheres which are porous smooth in nature and thus show good floating properties in gastric fluid. Microballoons release the drug in controlled manner at the targeted site. Microballoons are spherical empty vesicles without core and that can remain buoyant in gastric region for prolong period of time without irritation in gastrointestinal tract. Multiparticulate particles having a low density system that can efficiently prolong the gastric retention time of the drugs, thus enhanced bioavailability and thus improve the dosing frequency. These are less soluble at higher pH environment. As microballoons delivery systems provide longer retention in gastric pH and enhance the solubility of drugs that are less soluble in high pH environment. The formation of cavity inside the microballoons depend on the preparation, temperature and the surface smoothness determine the floatability and the release rate of microballoons. Keywords: Microballoons, Gastro retentive drug delivery system, Hollowspheres, Controlled release

scholarly journals Three-Dimensionally Ordered Macroporous-Mesoporous Bioactive Glass Ceramics for Drug Delivery Capacity and Evaluation of Drug Release

2020 ◽  
Author(s):  
Reedwan Bin Zafar Auniq ◽  
Namon Hirun ◽  
Upsorn Boonyang
Keyword(s):  
Drug Release ◽  
Bioactive Glass ◽  
Drug Loading ◽  
Diffusion Mechanism ◽  
Sol Gel ◽  
Glass Ceramics ◽  
Fickian Diffusion ◽  
Ordered Macroporous ◽  
Mesoporous Bioactive Glass

Bioactive glass ceramics (BGCs) have been used in orthopedic and dentistry due to having better osteoconductive and osteostimulative properties. This study aimed to evaluate and compare the drug release properties of two different BGCs; 45S5 and S53P4. The BGCs were composed with four phases of SiO2 – CaO – Na2O – P2O5 system, synthesized by sol–gel method using dual templates; a block-copolymer as mesoporous templates and polymer colloidal crystals as macroporous templates, called three-dimensionally ordered macroporous-mesoporous bioactive glass ceramics (3DOM-MBGCs). In vitro bioactivity test performed by soaking the 3DOM-MBGCs in simulated body fluid (SBF) at 37°C. The results indicated that, the 45S5 have the ability to grow hydroxyapatite-like layer on the surfaces faster than S53P4. Gentamicin drug was used to examine in vitro drug release properties in phosphate buffer solution (PBS). The amount of drug release was quantified through UV/Vis spectroscopy by using o-phthaldialdehyde reagent. S53P4 showed high drug loading content. The outcome of drug release in PBS showed that both S53P4 and 45S5 exhibited a slowly continuous gentamicin release. The resultant drug release profiles were fitted to the Peppas-Korsmeyer model to establish the predominant drug release mechanisms, which revealed that the kinetics of drug release from the glasses mostly dominated by Fickian diffusion mechanism.

Sinomenine-loaded microcapsules fabricated by phase reversion emulsification-drying in liquid method: An evaluation of process parameters, characterization, and released properties

2017 ◽  
Vol 33 (4) ◽  
pp. 382-396 ◽  
Author(s):  
Wen Zhang ◽  
Yan Gao ◽  
Ning Yang ◽  
Hua Zhang ◽  
Feng Zhang ◽  
...  
Keyword(s):  
Biological Activities ◽  
Drug Loading ◽  
Diffusion Mechanism ◽  
In Vitro Release ◽  
Spherical Shape ◽  
Fickian Diffusion ◽  
Anti Cancer ◽  
Methyl Thiazolyl Tetrazolium Assay ◽  
Natural Alkaloid

Sinomenine is a natural alkaloid with important biological activities (e.g. anti-cancer, anti-inflammatory, and anti-allergic). However, the unstability and short half-life absolutely limited its application to foods. Microencapsulation technology can offer a way to solve these issues. In this study, polylactic acid microcapsules loading sinomenine hydrochloride were fabricated by phase inversion emulsification-drying in liquid technique. The results showed that microcapsules had nice spherical shape, uniform particle size, and free flowing. The encapsulation efficiency was 89.2% and drug loading was 8.9% under the optimal conditions. In vitro release assays demonstrated that release of sinomenine from microcapsules was sustained and slow. Moreover, it was found that the sinomenine release fitted Fickian diffusion mechanism. The results of cytotoxicity study showed that sinomenine-loaded microcapsules were biocompatible. Sinomenine-loaded microcapsules could inhibit the growth of MDA-MB-231 cells using methyl thiazolyl tetrazolium assay. In summary, polylactide microcapsules exhibit excellent properties for sinomenine that can be used in drug or food industry.

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