Oil-in-Water Nanosized Emulsions for Drug Delivery and Targeting. Tamilvanan Shunmugaperumal. Читать онлайн. Newlib. NEWLIB.NET

Автор: Tamilvanan Shunmugaperumal
Издательство: John Wiley & Sons Limited
Серия:
Жанр произведения: Химия
Год издания: 0
isbn: 9781119585251
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onto the API incorporation patterns, final particle size distribution of dispersed oil droplets of the emulsion on different storage temperature conditions, etc., will be the subject of interest to be discussed in this chapter. It is to be informed to readers that the discussion of majority of the traditional excipients (oils, emulsifiers, and other excipients) can also be found from Chapter 4 wherein the classification of emulsions based on their generation appears.

Excipients Selected Examples
Oils Animal origin: Lanolin, squalene (shark liver oil)
Mineral origin: Paraffin light, paraffin oil, silicone oil, vaseline
Plant origin: Arachis oil, castor oil, corn oil, glycerol monostearate, medium‐chain monoglycerides, medium‐chain triglycerides, olive oil, sesame oil, soyabean oil, etc.
Emulsifiers: Amphoteric, anionic, neutral and nonionic Oil soluble: Cholesterol, cremophor RH, phospholipids (lipoid E 80) including phosphatidylcholine, phosphatidylethanolamine, sphingomyelin, etc.
Water soluble: Miranol C 2 M (disodium cocoamphodiacetate) Miranol MHT [(1H‐imidazolium, 4,5‐dihydro‐1‐(carboxymethyl)‐1‐(2‐hydroxyethyl)‐2‐undecyl‐, hydrogen sulfate (salt), monosodium salt)] Poloxamer [(poly(ethylene glycol)‐block‐poly(propylene glycol)‐block‐poly(ethylene glycol)] 188 and 407 Polysorbate/Tween 20 {2‐[2‐[3,4‐bis(2‐hydroxyethoxy)oxolan‐2‐yl]‐2‐(2‐hydroxyethoxy)ethoxy]ethyl dodecanoate} Polysorbate/Tween 80 {2‐[2‐[3,5‐bis(2‐hydroxyethoxy)oxolan‐2‐yl]‐2‐(2‐hydroxyethoxy)ethoxy]ethyl (E)‐octadec‐9‐enoate} Transcutol P (diethylene glycol monoethyl ether) Tyloxapol [4‐(1,1,3,3‐tetramethylbutyl)phenol polymer with formaldehyde and oxirane] TPGS (tocopheryl polyethylene glycol succinate)
Emulsifiers: Cationic Lipid: DMPE, DOTAP, oleylamine, stearylamine
Polysaccharide: Chitosan
Miscellaneous α‐Tocopherol, EDTA, glycerin, methylparaben, propylparaben, sorbitol, thiomersal, xylitol

      In general, the o/w nanosized emulsion should be formulated with compatible vehicles and additives. The components of internal (dispersed oil droplets) and external (aqueous continuous medium) phases of nanosized emulsions should be chosen to confer enhanced solubility and stability to the incorporated therapeutically active lipophilic API. In principle, the function of selected excipients should not only be limited to improve the overall physical stability of the emulsions or enhance the API's solubility but also they should contribute to influence the biofate or therapeutic index of the incorporated API after administration via parenteral, ocular, percutaneous, and nasal routes. The general considerations concerning excipient selection and optimum concentrations mainly in relation to the oils, emulsifiers, and miscellaneous excipients are presented comprehensively below.

      At the time of preformulation studies, the solubility data of APIs need to be generated in the different oil selected, that too either alone or in combination of one oil with other oils in a definite ratio. Two more important points should be kept in mind before selecting the oil or oil combination. First point is compatibility of the oil or oil combination not only with other formulation excipients but also with the site of applications, i.e., ocular/skin tissues. Second point is related to auto‐ or self‐oxidation potential of oil or oil combination during and after emulsion manufacturing, because oils are triglycerides and are prone to auto‐ or self‐oxidation over the emulsion's processing and storage time periods. To minimize or to eliminate some extent the auto‐ or self‐oxidation, the additional excipient recommended to include in the emulsion formula is antioxidants, especially α‐tocopherol in the concentration range from 0.001 to 0.002% w/w.

      Not only the chemical nature of emulsifiers but also their concentration used determine the type of emulsion produced. For example, the spontaneously forming thermodynamically