The title of this thesis “Synthesis and Characterization of Drug Carrier Based on Polysaccharides” clearly reflects the objective, which is an approach towards preparation of excipients, defined as ‘the substance used as a medium for giving a medicament’, that is to say with simply the functions of an inert support of the active principle or principles.
Okra gum, obtained from the fruits of Hibiscus esculents, is a polysaccharide consisting of D-galactose, L-rhamnose and L-galacturonic acid. It is used as a binder. In studies okra gum has been evaluated as a binder in paracetamol tablet formulations. These formulations containing okra gum as a binder showed a faster onset and higher amount of plastic deformation than those containing gelatin. The crushing strength and disintegration times of the tablets increased with higher binder concentration, while their friability decreased. Although gelatin produced four tablets with higher crushing strength, okra gum produced tablets with longer disintegration times than those containing gelatin. It was finally concluded from the results that okra gum may be a useful hydrophilic matrixing agent in sustained drug delivery system. Various strategies were developed in order to overcome these issues, offering the opportunity to tailor the physical and chemical properties of okra gum thus yielding materials that may find a wide range of applications.
Extraction and purification of okra gum was carried out from okra pods. Followed by carboxymethylated and phosphorylation of extracted okra gum, which was carried out along with optimization of reaction parameter of the primary derivatives that is carboxymethylated okra gum and hydroxyl propyl okra phosphate, followed by drug carriers preparation. By the second modification carboxymethylated okra gum and hydroxyl propyl okra phosphate were carried out by cross linking acrylic acid, N, N-methylene acryl amide, hydroxyethyl methacrylate (HEMA) respectively synthesized cross-linked polymer were further investigated as drug carriers by formulating as tablet for sustained drug release. The drug release of different formulations were measured in relation to time and also compared with the standard drugs. Further mathematical modeling was implemented to know the order of release behavior of formulated tables.
Table of Contents
Abstract
Chapter- 1
1.0 Introduction
1.1 Monosaccharide
1.1.1 Classification of monosaccharide
1.1.1.1 Trioses
1.1.1.2 Tetroses
1.1.1.3 Pentoses
1.1.1.4 Hexoses
1.2 Function in biology
1.2.1 Energy respiration
1.2.2 Aerobic respiration
1.2.3 Anaerobic respiration
1.3 Fermentation
1.3.1 Allose
1.3.2 Altrose
1.3.3 Galactose
1.3.4 Gulose
1.3.5 Idose
1.3.6 Mannose
1.4 A cyclic form of glucose
1.5 Production
1.5.1 Biosynthesis
1.5.2 Commercial
1.5.3 Physical properties
1.5.4 Fructose
1.5.5 Chemical properties
1.5.6 Physical and functional properties
1.5.7 Fructose solubility with crystallization
1.5.8 Food source
1.5.9 Galactose
1.5.10 Structure and isomerism
1.5.11 Sources
1.5.12 Glycolipids
1.5.13 Glycoprotein
1.6 Polysaccharides
1.6.1 Task of polysaccharide
1.6.2 Structure of polysaccharide
1.7 Example of polysaccharide
1.7.1 Starch
1.7.2 Glycogen
1.7.3 Cellulose
1.7.4 Chitin
1.8 Plant polysaccharides
1.8.1 Pectin
1.9 Gums and it’s classification
1.9.1 Classification:
1.9.2 Natural gums:
1.9.3 Tamarind gum
1.9.4 Locust bean gum
1.9.5 Tara gum
1.9.6 Honey locust bean gum
1.9.7 Guar gum
1.9.8 Okra gum
1.9.9 Khaya gum
1.10 What are gums and mucilage’s?
1.10.1 Advantages of natural gums and mucilage’s in pharmaceutical sciences
1.10.2 Disadvantages of natural gums and mucilage’s
1.10.3 Classification of gums and mucilage’s
1.10.4 Applications of gums and mucilage’s
1.10.5 Application in the food industry
1.10.6 Pharmaceutical applications
1.10.7 Industrial uses
1.11 Isolation and purification of gums/mucilage’s
1.11.1 Characterization / standardization of gums and mucilage’s
1.11.2 Pharmacopoeial standard specifications of gums and mucilage’s
1.12 Reasons for developing new excipients
1.13 Modification of existing gums and mucilage’s
1.14 Purpose of modification
1.14.1 To target at a particular site:
1.14.2 To make the polymers more heat or moisture-resistant:
1.14.3 To alter its solubility, more sustainable:
1.14.4 To make it more flexible, more transparent, and more compatible and/or biodegradable
1.14.5 Biopolymers may also have unique features like antimicrobial effects, which can be utilized to add value to end products:
1.14.6 To reduce the toxicity:
1.15 Derivatives of natural gums
1.15.1 Carboxyl derivatives
1.15.2 Hydroxyethyl derivatives
1.15.3 Vinyl-functioned derivatives
1.15.4 Cationic derivatives
1.15.5 Amphoteric derivatives
1.15.6 Hydrophobic derivatives
1.16 Methodological approaches and categorization of polymeric modification techniques.
1.16.1 Polymer grafting
1.16.2 Chemical grafting
1.16.3 Grafting by chemical routes
1.17 With fenton’s reagent (Fe2+ / H2O2)
1.18 Cross linking
1.19 Conventional pharmacotherapy
1.20 Controlled release methods
1.21 Time - controlled: modified - release formulation
1.21.1 Extended-release formulation
1.21.2 Sustained release formulation
1.21.3 Pulsatile - release formulation
1.21.4 Delivery device that releases the drug
1.21.5 Delayed - release formulation
1.22 Controlled distribution
1.23 Polymers used for controlled-drug release
1.23.1 What is drug?
1.23.2 What are excipients?
1.23.3 Pharmaceutical formulation
1.23.4 Drug delivery route
1.23.5 Drug delivery systems
1.24 Conventional drug therapy
1.25 Sustained release formulations
1.25.1 Advantages of sustained release dosage forms
1.25.2 Disadvantages of sustained - release dosage forms
1.26 Tablets as a dosage form
1.26.1 Conventional routes of drug administration
1.27 Types of tablets
1.27.1 Compressed tablets:
1.27.2 Sugar coated tablets:
1.27.3 Film - coated tablets:
1.27.4 Multiple compressed tablets:
1.27.5 Controlled Released Tablet:
1.27.6 Effervescent tablets:
1.28 Tablet ingredients
1.29 In - vitro dissolution testing in pharmaceutical analysis
1.29.1 Dissolution testing in pharmaceutical analysis
1.30 Dissolution
1.30.1 Dissolution method parameters
1.30.2 Active pharmaceutical ingredient (API)
1.30.3 Dosage Form
1.30.4 Media
1.30.5 Visual observations
1.30.6 Mathematical models for drug Delivery
1.31 Analysis
1.31.1 In-vivo testing in pharmaceutical analysis
1.32 Post-marketing studies
1.33 Principles of examination techniques used throughout the present study
1.33.1 Fourier transform infra - red spectroscopy analysis (FTIR)
1.33.2 Powder x-ray diffraction (XRD)
1.33.3 Scanning electron microscope (SEM)
Chapter - 2
2.0 Extraction of okra gum and its primary modification
2.1 Introduction
2.2 Isolation of mucilage from lady’s finger by a conventional procedure
2.2.1 Petroleum ether extract
2.2.2 Chloroform extract
2.2.3 Ethyl acetate extract
2.2.4 Methanol extract
2.3 Chemistry of okra gum
2.4 Selection of okra
2.5 Physico-chemical characterization of okra gum
2.5.1 Identification tests for gums
2.5.2 Solubility test
2.5.3 pH determination
2.5.4 Moisture content
2.5.5 Viscosity
2.5.6 Fourier transform infrared (FTIR)
2.6 Chemical modification of okra gum
Part -1 : Extarction of okra gum
2.7 Experimental method
2.7.1 Chemicals
2.8 Methods
2.8.1 Extraction of okra gum
2.8.2 Purification of okra gum
2.8.3. Moisture content
2.8.4 pH determination
2.8.5 Solubility test
2.8.6 Viscosity
2.9 Characterization of extracted okra gum
2.9.1 FTIR spectroscopy of okra gum
Part-2 : Preparation of Okra Phosphate
2.10 Preparation of Okra Phosphate
2.10.1 Purification of okra phosphate
2.10.2 FTIR spectrums of okra phosphate:
Part-3: Preparation of Hydroxypropyl Okra Phosphate from Okra Phosphate
2.11 Preparation of hydroxypropyl okra phosphate from okra phosphate
2.11.1 Purification of hydroxy propyl okra phosphate
2.11.2 Degree of substitution of hydroxylpropyl okra phosphate
2.12 Optimization study parameters of hydroxyl propyl okra phosphate
2.12.1 Effect of NaOH
2.12.2 Effect of temperature
2.12.3 Effects of 3-chloropropionic acid
2.12.4 Effects of time
2.13 FTIR spectrums of hydroxypropyl okra phosphate:
Part-4: Carboxymethylated of okra gum
2.14 prepration of carboxymethylated of okra gum
2.15 Results and discussion
2.15.1 An optimization study of carboxymethylated reaction parameters
2.16 FTIR Spectroscopy of carboxymethylated of okra gum
2.17 summary of okra gum and its primary derivatives
2.18 Conclusion
Chapter - 3
Hydrogel preparation
3.1 Introduction
3.2 Literature review gums grafted with acrylic acid or its derivatives
Part-1: Preparation of hydrogel from hydroxypropyl okra phosphate by using acrylic amide as monomer
3.3 Materials and methods
Table 3.1: Raw Materials
3.4 Methods
3.4.1 Preparation of hydrogel from hydroxypropyl okra phosphate by using acrylic amide as monomer (Hydrogel-1).
3.5 Properties of Hydrogels:
3.5.1 Swelling property:
3.5.2 Mechanical properties:
3.5.3 Biocompatible properties:
3.6 Characterization of derived hydrogel
3.6.1 Moisture content
3.6.2 pH determination
3.6.3 Solubility test
3.6.3 Viscosity
3.7 Degree of substitution of hydrogel
3.8 FTIR spectroscopy
3.9 Thermo gravimetric analysis
3.10 Scanning electron microscopy
3.11 Powder X-Ray Diffraction
3.12 Method of partical size distribution
3.13 Result and discussion:
3.13.1 Optimization study parameters of hydroxyl propyl okra phosphate cross-linking with acrylic amide monomer (Hydrogel-1)
3.13.2 Effect of CAN:
3.13.3 Effect of temperature:
3.13.4 Effects of acrylic amide:
3.13.5 Effects of time:
3.14 Water absorption studies:
3.14.1 The water absorption was calculate:
3.14.2 Swelling ratio:
3.15 FTIR spectrums
3.15.1 Hydroxylsethyl okra phosphate by cross-linking with acrilcy amide
3.15.2 Thermo gravimetric analysis hydrogel-1
3.15.3 SEM (scanning electron microscopy)
3.15.4 Powder X-ray diffraction
3.15.5 Partical size distribution
Part-2 : Preparation of hydrogel from carboxymethylated okra gum by using haydroxyethyl methacrylate (HEMA) as monomer (Hydrogel-2)
3.16 Preparation of hydrogel from carboxymethylated okra gum by using haydroxyethyl methacrylate (HEMA) as monomer (Hydrogel-2)
3.16.1 Properties of hydrogels:
3.16.2 Mechanical properties:
3.17 Characterization of derived hydrogel
3.17.1 Moisture content
3.17.2 pH determination
3.17.3 Solubility test
3.17.4 Viscosity
3.18 Degree of substitution of hydrogel 2
3.19 FTIR spectroscopy
3.19 Thermo gravimetric analysis
3.20 Scanning electron microscopy
3.21 Powder X-Ray Diffraction
3.22 Method of partical size distribution
3.23 Result and Discussion:
3.24 Optimization study parameters of carboxymethylated okra gum cross-linking with haydroxyethyl methacrylate (HEMA) monomer (Hydrogel-2)
3.24.1 Effect of CAN:
3.24.2 Effect of temperature:
3.24.3 Effects of haydroxyethyl methacrylate:
3.24.4 Effects of time:
3.25 Water absorption studies:
3.25.1 The water absorption was calculated by:
3.26 Swelling ratio:
3.27 FTIR spectrums
3.27.1 Hydroxylsethyl okra phosphate by cross-linking with acrilcy amide
3.27.2 Carboxymethylated okra gum by cross-linking hydroxyethyl methacrylate
3.28 SEM (scanning electron microscopy)
3.29 Thermo gravimetric analysis hdrogel-2
3.30 partical size distribution analysis hydrogel-2
Conclusion:
Chapter - 4
Application of okra gum and its derivatives
4.0 Introduction
4.1 Pharmaceutical dosage forms
4.1.1 Importance of dosage forms
4.2 Solid dosage form
4.2.1 Tablets
4.2.2 Tablet ingredients
4.2.3 Additives are classified according to functions as follow
4.3 Method of preparation of compressed tablets
4.4 Materials and method
4.5 Drug profile
4.5.1 Diclofenace sodium: (Phenyl acetic acid derivative NSAID)
4.6 Methods
4.7 Preparation of tablets
4.8 Evaluation of granules
4.8.1 Angle of repose
4.8.2 Bulk density
4.9 Evaluation of tablets
4.9.1 Hardness
4.9.2 Uniformity weight
4.9.3 Friability
4.9.4 Uniformity of drug content
4.9.5 In-vitro drug release studies
4.10 Mathematical models for drug release studies
4.10 Results and discussion
Part – 1 Cross-linked hydroxypropyl okra phosphate with acrylic amide
4.10.1 Angle of repose
4.11 Bulk density
4.12 Hardness
4.13 Friability
4.14 Uniformity of drug content
4.15.1 The standard curve of diclofenac sodium drug
4.16.2 Cumulative % of drug release
4.16.2 Mathematical models for drug Delivery
Part – 2 Cross-linked Carboxymethyl okra gum with hydroxyethyl methacrylatele
4.10 Results and discussion
4.10.1 Angle of repose
4.11 Bulk density
4.12 Hardness
4.13 Friability
4.14 Uniformity of drug content
4.15 Uniformity of drug content
4.16 Zero order release Cross-linked Carboxymethyl okra gum
4.17 Higuchi model of Cross-linked Carboxymethyl okra gum
4.18 Mathematical models of Cross-linked hydroxypropyl okra
4.19 Mathematical models of Cross-linked Carboxymethyl okra gum okra
4.20 Conclusion
Chapter: 5
5.1 Conclusion
5.2 Future aspects:
Research Goal and Topics
The primary objective of this thesis is to synthesize and characterize drug carriers based on polysaccharides, specifically focusing on Okra gum, to evaluate their effectiveness as excipients in pharmaceutical formulations for controlled and sustained drug delivery.
- Extraction and modification of Okra polysaccharides (e.g., carboxymethylation and phosphorylation).
- Physico-chemical characterization using advanced techniques like FTIR, XRD, and SEM.
- Preparation of hydrogels from modified okra derivatives using cross-linking techniques.
- Application of these modified gums as binder agents in sustained-release tablet formulations (e.g., with Diclofenac sodium).
- Mathematical modeling of drug release kinetics to determine the retardant properties of the formulations.
Excerpt from the book
1.1 Monosaccharide
Structure of monosaccharide may be (1) Straight or open-chain (2) Cyclic or ring structure.
Here two ends remain separate, so it calls open-chain structure in these six carbon atoms of glucose kept in a straight chain. The types of, open-chain structure (a) Structure given by fitting and Baeyer (b) Structure given by Fischer called fishers projection formula. Fishers projection prepared by Hermann Fischer in 1891[1]. This projection is introduced for illustration of carbohydrates; it is used by chemists for organic, inorganic chemistry.
Summary of Chapters
Chapter- 1: Covers the fundamental concepts of carbohydrates, specifically monosaccharides and polysaccharides, their chemical structures, biological functions, and their common classification as pharmaceutical excipients.
Chapter - 2: Discusses the systematic extraction of okra gum from pods, its chemical modification through phosphorylation and carboxymethylation, and the detailed physico-chemical characterization of these derivatives.
Chapter - 3: Details the preparation of hydrogels using the modified okra derivatives by cross-linking with monomers like acrylic amide and hydroxyethyl methacrylate, including the optimization of reaction parameters.
Chapter - 4: Focuses on the pharmaceutical application of the synthesized polymers as binders in Diclofenac sodium tablet formulations, evaluating their impact on drug release kinetics through various in-vitro testing methods.
Keywords
Okra gum, Polysaccharides, Drug Delivery Systems, Sustained Release, Hydrogel, Excipients, Carboxymethylation, Phosphorylation, Diclofenac Sodium, Polymer Grafting, Tablets, Dissolution Testing, FTIR, In-vitro studies.
Frequently Asked Questions
What is the core focus of this research?
The core focus is the synthesis and characterization of natural polysaccharide-based drug carriers, specifically using Okra gum, to improve pharmaceutical delivery systems.
What are the primary themes of the work?
The work explores extraction processes, chemical modifications (grafting/cross-linking), characterization, and the application of these modified polymers in sustained-release pharmaceutical tablets.
What is the main objective or research question?
The main objective is to overcome limitations of natural gums (like batch variability and uncontrolled hydration) by modifying them to create stable, effective drug delivery matrices.
What scientific methods were employed?
The study utilized solid-liquid extraction, chemical synthesis for modifications (etherification/cross-linking), and analytical techniques including FTIR, XRD, SEM, and dissolution study modeling.
What topics are discussed in the main part?
The main body treats the chemical profiling of monosaccharides/polysaccharides, extraction parameters of Okra gum, preparation of hydrogels, and the performance analysis of drug-loaded tablets.
Which keywords characterize the work?
Keywords include Okra gum, polysaccharides, sustain-release, hydrogels, polymer modification, and Diclofenac sodium formulation.
How is the chemical modification of Okra gum evaluated?
Modification success is determined through FTIR spectroscopy, degree of substitution calculations, and thermal analysis (TGA) to confirm the structural changes in the polymer backbone.
What is the benefit of the hydrogels developed in the research?
These developed hydrogels provide controlled drug release by forming specific network structures that protect the drug and allow for tunable release kinetics based on environmental stimuli.
- Arbeit zitieren
- Prof. (Dr.) Nirmal K. Patel (Autor:in), Dr. Savan H. Patel (Autor:in), 2022, Synthesis and characterization of drug carrier based on polysaccharides, München, GRIN Verlag, https://www.grin.com/document/1311192
