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Abstract
ABSTRACT
PART ONE
Formulation and Evaluation of Diclofenac Sodium-Entrapped Niosomes As a Topical Drug Delivery System.
CHAPTER ONE
Preparation and In-Vitro Evaluation of Diclofenac Sodium Niosomal Formulations.
1. Niosomes were prepared with a series of non-ionic surfactants and co-surfactants, with or without cholesterol (Chol) and charged lipids. The prepared niosomes were evaluated and the effect of variables like lipid composition, total lipid concentration, drug concentration, method of preparation and incorporation of co-surfactants on the entrapment efficiency (EE) and in-vitro release rate of DCS from was investigated.
2. It was found that niosomes formed of Span 60 gave the highest EE, increasing the Chol concentration resulted in an increase in the EE % of niosomes. It was found that increasing the total lipid concentration resulted in increasing the EE expressed as (%). Increasing the concentration of DCS was accompanied by a slight increase in the EE expressed as (%)
3. Incorporation of charge-inducing agents caused a marked increase in the EE (%).
4. Niosomes prepared by EIM and REV resulted in a marked increase in the EE (%) compared to those prepared by HSM. It was demonstrated that the use of co-surfactants caused an increase in the EE (%).
5. The in-vitro release of DCS from different niosomal formulations was studied. Niosomes prepared from Span 40 and Span 60 showed a slower release rate. It was found that Chol reduced the percentage DCS released from niosomes, Introduction of charge-inducing agents caused a further reduction of release rate.
6. It was observed that niosomes prepared by HSM showed a slower release rate than those prepared by EIM and REV. The incorporation of co-surfactants resulted in a greater decrease in the release rate of DCS.
CHAPTER TWO
Biological Evaluation of Diclofenac Sodium-Entrapped Niosomes After Topical Administration.
1. Niosomes prepared by HSM using Span 60/Tween 60/Chol in a molar ratio of 25:25:50 were chosen and incorporated in different gelling agents like carbopol 934 and carboxymethyl cellulose sodium (CMC Na) with different concentration.
2. The effect of gelling agent concentration on the permeation of DCS from niosomal gels through rabbit skin was studied. It was found that increasing the gelling agent concentration resulted in a reduction in the amount of drug permeated through the rabbit skin.
3. Incorporation of DCS-entrapped niosomes into gels resulted in a marked decrease in the amount of drug permeated through the rabbit skin.
4. Storage of niosomal formulations for a period of 8 weeks at different storage conditions was studied. The refrigerating temperature was found to be the most suitable temperature for the storage of niosomes.
5. The niosomal gel formulations of diclofenac sodium improved the topical anti-inflammatory, analgesic activities, compared to the plain drug gel and marketed gel formulations.
PART TWO
Formulation and Evaluation of Piroxicam-Entrapped Niosomes As an Oral Drug Delivery System
CHAPTER ONE
Preparation and In-Vitro Evaluation of Piroxicam Niosomal Formulations.
1. Niosomes prepared with Span 40 and Span 60 showed the highest EE, It was found that increasing the concentration of Chol resulted in an increase in the EE % of niosomes.
2. It was observed that increasing the total lipid concentration resulted in an increase in the EE expressed as (%). Increasing the concentration of PRX was accompanied by an increase in the EE%.
3. Incorporation of charge-inducing agents in caused a marked increase in the EE %. Niosomes prepared by HSM resulted in an increase in the EE compared to those prepared by OSIM and REV.
4. Niosomes prepared from Span 40 and Span 60 showed a slower release rate. Increasing the concentration of Chol caused a marked reduction of the percentage PRX released from niosomes. Introduction of charge- inducing agents caused a further reduction of release rate.
5. It was demonstrated that niosomes prepared by HSM showed slower release rate than those prepared by OSIM and REV.
CHAPTER TWO
Biological Evaluation of
Piroxicam-Entrapped Niosomes After Oral Administration
1. Niosomes prepared with Span 40/Chol/ SA (45:45:10) were selected as a model formulation for the pharmacological evaluation of piroxicam niosomes.
2. The pharmacological evaluation was based on determining the anti-inflammatory activity of piroxicam-loaded niosomes using carrageenan rat hind paw oedema method and analgesic activity using hot plate test.
3. It was observed that the ulceration potential of the drug was reduced considerably when PRX entrapped niosomes were administered orally.
الموجز الإنجليزي :
Controlled Release Formulations of Certain
Anti-inflammatory Drugs.
Part (I): Formulation and Evaluation of Diclofenac Sodium-Entrapped Niosomes As a Topical Drug Delivery System.
Chapter (I): Preparation and In-Vitro Evaluation of Diclofenac Sodium Niosomal Formulations.
Diclofenac sodium-entrapped niosomes were prepared with a series of non-ionic surfactants and co-surfactants, with or without cholesterol and charged lipids. The prepared niosomes were evaluated and the effect of variables like lipid composition, total lipid concentration, drug concentration, method of preparation and incorporation of co-surfactants on the entrapment efficiency and in-vitro release rate of DCS from was investigated.
Chapter (II): Biological Evaluation of Diclofenac Sodium-Entrapped Niosomes After Topical Administration.
In this chapter niosomes prepared by HSM using Span 60/Tween 60/Chol in a molar ratio of 25:25:50 were chosen and incorporated in different gelling agents like carbopol 934 and carboxymethyl cellulose sodium (CMC Na) with different concentration to study the topical application of niosomes. It was found that Incorporation of DCS-entrapped niosomes into gels resulted in a marked decrease in the amount of drug permeated from gels through the abdominal rabbit skin.
Part (II): Formulation and Evaluation of Piroxicam-Entrapped Niosomes As an Oral Drug Delivery System.
Chapter (I): Preparation and In-Vitro Evaluation of Piroxicam Niosomal Formulations.
This chapter covers the preparation of niosomes of piroxicam with series of non-ionic surfactants. Entrapment efficiency and In-vitro release from niosomes was influenced by lipid composition, cholesterol content and incorporation of charge inducing agents, total lipid concentration, drug concentration, method of preparation (HSM, OSIM and REV) and incorporation of co-surfactants.
Chapter (II): Biological Evaluation of
Piroxicam-Entrapped Niosomes After Oral Administration
In this chapter, Niosomes prepared with Span 40/Chol/ SA (45:45:10) were selected as a model formulation for the pharmacological evaluation of piroxicam niosomes. It was found that the incorporation of PRX into niosomes improved the anti-inflammatory and analgesic activities of the drug. It was observed that the ulceration potential of the drug was reduced considerably when PRX entrapped niosomes were administered orally.