Overcoming poor oral bioavailability using nanoparticle formulations – opportunities and limitations

Desai, Preshita; Date, Abhijit A.; Patravale, Vandana

doi:10.1016/j.ddtec.2011.12.001

Cited by 161 publications

(108 citation statements)

References 45 publications

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“…33 In brief, SDC and phospholipids were mixed in a weight ratio of 4:6 and dissolved in a methanol/methylene chloride mixed solution (1:1, v:v) and then dried with a rotary evaporator. The resulting film was hydrated with a polymer solution for 1 hour and then diluted with the same solution to obtain MM suspensions with concentrations of 1,10,20,30,40,50,60,70, and 80 mg/mL. An excess amount of FB was added to the 5 mL MM suspensions, which were then shaken in a water bath shaker at 37°C for 60 hours until equilibrium was reached.…”

Section: Effects Of Hydrophilic Polymers On Solubilization Of Mms To Fbmentioning

confidence: 99%

“…It was estimated that sales of oral formulations of drugs in the United States alone would reach $56.7 billion in 2012. 1 Thus, the development of novel drugs and technologies that are effective when administered orally is a mainstay of pharmaceutical research. However, approximately 40% of the drugs in development and approximately 60% of the drugs coming directly from synthesis are poorly soluble.…”

Section: Introductionmentioning

confidence: 99%

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Bile salt/phospholipid mixed micelle precursor pellets prepared by fluid-bed coating

Dong¹,

Xie²,

Qi³

et al. 2013

IJN

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Bile salt/phospholipid mixed micelles (MMs) are potent carriers used for oral absorption of drugs that are poorly soluble in water; however, there are many limitations associated with liquid formulations. In the current study, the feasibility of preparing bile salt/ phospholipid MM precursor (preMM) pellets with high oral bioavailability, using fluid-bed coating technology, was examined. In this study, fenofibrate (FB) and sodium deoxycholate (SDC) were used as the model drug and the bile salt, respectively. To prepare the MMs and to serve as the micellular carrier, a weight ratio of 4:6 was selected for the sodium deoxycholate/ phospholipids based on the ternary phase diagram. Polyethylene glycol (PEG) 6000 was selected as the dispersion matrix for precipitation of the MMs onto pellets, since it can enhance the solubilizing ability of the MMs. Coating of the MMs onto the pellets using the fluid-bed coating technology was efficient and the pellets were spherical and intact. MMs could be easily reconstituted from preMM pellets in water. Although they existed in a crystalline state in the preMM pellets, FB could be encapsulated into the reconstituted MMs, and the MMs were redispersed better than solid dispersion pellets (FB:PEG = 1:3) and Lipanthyl ® . The redispersibility of the preMM pellets increased with the increase of the FB/PEG/micellar carrier. PreMM pellets with a FB:PEG:micellar carrier ratio of 1:1.5:1.5 showed 284% and 145% bioavailability relative to Lipanthyl ® and solid dispersion pellets (FB:PEG = 1:3), respectively. Fluid-bed coating technology has considerable potential for use in preparing sodium deoxycholate/phospholipid preMM pellets, with enhanced oral bioavailability for poorly water-soluble drugs.

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Section: Effects Of Hydrophilic Polymers On Solubilization Of Mms To Fbmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Bile salt/phospholipid mixed micelle precursor pellets prepared by fluid-bed coating

Dong¹,

Xie²,

Qi³

et al. 2013

IJN

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“…An oral film or strips are manufactured as a large sheet and then cut into individual dosage unit for packaging (Desai et al, 2012). Oral film used for local action in mouth such as local anesthetic for toothaches, oral ulcer, cold sores or teething etc.…”

Section: Introductionmentioning

confidence: 99%

Oral Films: A Comprehensive Review

et al. 2016

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In the late 1970s, rapid disintegrating drug delivery system was developed as an alternative to capsules, tablets and syrups for geriatric and pediatric patients having problems in swallowing. To overcome the need, number of orally disintegrating tablets which disintegrate within one minute in mouth without chewing or drinking water were commercialized. Then later, oral drug delivery technology had been improved from conventional dosage form to modified release dosage form and developed recently rapid disintegrating films rather than oral disintegrating tablets. Oral disintegrating film or strips containing water dissolving polymer retain the dosage form to be quickly hydrated by saliva, adhere to mucosa, and disintegrate within a few seconds, dissolve and releases medication for oro-mucosal absorption when placed in mouth. Oral film technology is the alternative route with first pass metabolism. This review give a comprehensive detail of materials used in ODF, manufacturing process, evaluation tests and marketed products.Mahboob et al., International Current Pharmaceutical Journal, November 2016, 5(12): 111-117http://www.icpjonline.com/documents/Vol5Issue12/03.pdf

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“…This resulted in our investigation of producing nanoemulsion as a potential approach to improve tocols solubility. The developed nanoemulsion will be used to produce microparticle for oral administration as it is considered as the most desirable route due to its convenience (Desai et al, 2012). Nanoemulsion also serves as an effective oxygen barrier that enhances the viability of the compound in the acidic medium of the digestive system of the stomach (De Vos et al, 2012).…”

mentioning

confidence: 99%