Saravana Kumar, T (2021) Formulation Optimization and Characterization of Self-Micro Emulsifying Drug Delivery System of Ivermectin. Masters thesis, College of Pharmacy, Madras Medical College, Chennai.
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Abstract
The number of potential drug candidates that have poor aqueous solubility is progressively increasing. Accordingly, the problem has become dominant in the pharmaceutical industry. • Formulation plays a major role in determining the rate and extent of absorption of such drugs from GIT. There are a number of drug strategies that could be used to improve the bioavailability of these drugs, either by increasing the dissolution rate or by presenting the drug in solution in the intestinal lumen. But most of the techniques used were with limitation of reproducibility, and stability. • Among different approaches that have developed to enhance the aqueous solubility, the use of the self-Micro emulsifying drug delivery systems (SMEDDS) has drawn considerable attention and ultimately therapeutical and commercial success in the oral delivery of Poorly water soluble drug delivery system (PWSDs). • They provide the PWSDs in the form of solubilized microdispersions. Consequently, the rate-limiting step of the PWSDs dissolution is bypassed. Nonetheless, SMEDDS are typically filled in soft gelatin capsules, which might cause the following problems: interaction with the capsule shell, instability, higher production cost and possible drug precipitation. Therefore, alternative formulation strategies, e.g. the inclusion of SMEDDS into a solid or semisolid dosage form, are desirable; nevertheless, very challenging. • These formulations can also enhance drug absorption by a number of ancillary mechanisms, including inhibition of P-glycoprotein- mediated drug efflux, inhibition of pre-absorptive metabolism by gut membrane- bound cytochrome enzymes and/or promotion of lymphatic transport, which delivers drug directly to the systemic circulation while avoiding hepatic first-pass metabolism, and by increasing GI membrane permeability. • Self-Micro emulsifying drug delivery system usually includes oil, non-ionic surfactant and co-surfactant, and the performance of these formulations depends upon the right combination of these. • Most of the oils have the limitation of drug solubility and thus large amount of surfactant and co-surfactant are incorporated in the SMEDDS formulation to solubilize the drug. • Toxicity of these surfactants is an independent issue, and is important with regard to the choice of surfactants so it is pertinent to compare the toxicity of non-ionic surfactants. • Co- surfactant e.g. ethanol, propylene glycol, these alcohols and other volatile co-solvents have the disadvantage of evaporation into the shells of the soft gelatin capsules in conventional SMEDDS leading to drug precipitation. • The absolute bioavailability of Ivermectin is approximately 56 %. Poor aqueous solubility, substrate to efflux mechanism of the GIT, high intestinal clearance and first-pass metabolism, are thought to be the main cause for the low systemic availability. It is a right candidate to formulate into a SMEDDS formulation. • The aim of the present study was to formulate, optimize and characterize stable self microemulsifying drug delivery system (SMEDDS) in order to enhance solubility as well as dissolution rate of this highly lipophilic drug, using single non-ionic surfactant with the use of a co-surfactant. FUTURE PLAN: ❖ Scale up studies of the optimized formulation. ❖ In vivo studies and in vitro – in vivo correlation studies. ❖ To study the Bio equivalence study to optimize further.
| Item Type: | Thesis (Masters) |
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| Additional Information: | 261911258 |
| Uncontrolled Keywords: | Formulation, Optimization, Characterization, Self-Micro Emulsifying Drug Delivery System, Ivermectin. |
| Subjects: | PHARMACY > Pharmaceutics |
| Depositing User: | Subramani R |
| Date Deposited: | 01 Nov 2022 17:11 |
| Last Modified: | 01 Nov 2022 17:11 |
| URI: | http://repository-tnmgrmu.ac.in/id/eprint/20891 |
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