Evaluation of cytotoxicity of oils used in coenzyme Q10 Self-Emulsifying Drug Delivery Systems (SEDDS)

Palamakula, Anitha; Khan, Mansoor A.

doi:10.1016/j.ijpharm.2003.12.010

Cited by 60 publications

(30 citation statements)

References 21 publications

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“…However, in some reports, the bioavailability has not increased even though the in vitro dissolution rate or emulsification rate has increased [17,18] . Although there are some reports about anaphylactic reactions to Cremophor, these reactions were observed during intravenous administration, but not during oral administration, based on cytotoxicity studies for SNEDDS oral formulations containing Cremophor [19,20] . Our previous studies [12,13] indicated that SNEDD preparations of vitamin A in semisolid and solid forms have improved emulsification and in vitro drug release characteristics.…”

Section: Discussionmentioning

confidence: 99%

Bioavailability Assessment of Vitamin A Self-Nanoemulsified Drug Delivery Systems in Rats: A Comparative Study

Taha

Ghorab²,

Zaghloul³

2007

Med Princ Pract

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Objectives: To assess and compare the bioavailability of three different oral dosage forms of vitamin A in rats. The formulations included vitamin A self-nanoemulsified drug delivery (SNEDD) optimized formulation-filled capsule (F1), vitamin A SNEDD optimized formulation compressed tablet (F2) and vitamin A oily solution-filled capsules without any additives (control, F3). Materials and Methods: Bioavailability was assessed after a single oral dose of the three formulations using three groups of rats, each group comprising 6 rats. Blood samples were collected at baseline and over the next 8 h. Plasma was separated and extracted to obtain the drug, which was measured by HPLC. Statistical data analysis was performed using the Student t test and ANOVA with p < 0.05 as the minimal level of significance. Results: From the pharmacokinetic parameters, both F1 and F2 showed improved bioavailability compared to F3. The values of AUC ± SD were 3,080.7 ± 190.2, 2,137.1 ± 130.5 and 1,485.2 ± 80.1 ng·h/ml for F1, F2 and F3, respectively. The T_max was 1 h in case of F1 and F2 as compared to 1.5 h for F3. The C_max ± SD was 799.5 ± 48.5, 656.2 ± 64.4 and 425.8 ± 33.1 for F1, F2 and F3, respectively. The increase in AUC, C_max and T_max was significant (p < 0.05). The bioavailability calculated from the AUC for F1 and F2 relative to F3 was 207.4 and 143.8%, respectively. The bioavailability increased almost twofold and 1.4 times for F1 and F2, respectively. Conclusions: The study showed that the newly developed vitamin A SNEDD formulations increased the rate and extent of drug absorption compared to the oily drug solution. The present investigation demonstrated that vitamin A SNEDD optimized formulations, either as filled capsules or as compressed tablets, were superior to its oily solution with regard to their biopharmaceutical characteristics.

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Section: Discussionmentioning

confidence: 99%

Bioavailability Assessment of Vitamin A Self-Nanoemulsified Drug Delivery Systems in Rats: A Comparative Study

Taha

Ghorab²,

Zaghloul³

2007

Med Princ Pract

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“…Several works have tested different administration routes for these oils and shown that they all are physiologically tolerable oils [20,21]. The selection of the oily phase of the nanoemulsion is very important because the solubility of the drug in the formulation is critically dependant on this factor [22,23]. From this point of view, IPM and Capmul MCM-L Ò were selected for a forthcoming screening due to their high ZnPc solubilization capacity.…”

Section: Resultsmentioning

confidence: 99%

A comparative study of a novel lipophilic phthalocyanine incorporated into nanoemulsion formulations: Photophysics, size, solubility and thermodynamic stability

et al. 2011

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“…Usually the excipients with GRAS status, such as naturally derived oils and medium chain triglycerides are chosen for SEDDS development. However, many oils and surfactants may show cytotoxic effects if not used in low concentrations (Palamakula & Khan, 2004). To investigate cytotoxic effects of DES/AOT-SEDDS-F4 and DES/AOT-SEDDS-F15 a cell viability assay of a Caco-2 monolayer was determined.…”

Section: Enzymatic Stability Studiesmentioning

confidence: 99%

Development andin vitroevaluation of an oral SEDDS for desmopressin

et al. 2016

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Context: Self-emulsifying drug delivery systems (SEDDS) are among most promising tools for improving oral peptide bioavailability. Objective: In this study, in vitro protective effect of SEDDS containing desmopressin against presystemic inactivation by glutathione and a-chymotrypsin was evaluated. Materials and methods: The partitioning coefficient (log P) of desmopressin was increased via hydrophobic ion pairing using anionic surfactants. Solubility studies were performed to select the appropriate solvents for SEDDS preparation. Subsequently, droplet size and emulsification properties of 22 SEDDS formulations were evaluated. Moreover, the peptide-surfactant complex was dissolved in two chosen SEDDS formulations. Finally, SEDDS containing desmopressin were characterized regarding lipase stability, toxicity, and in vitro protective effect toward glutathione and a-chymotrypsin. Results: Desmopressin log P was increased from initial À6.13 to 0.33 using sodium docusate. The resulting desmopressin docusate complex (DES/AOT) was incorporated in two different SEDDS formulations, containing Capmul 907 P as main solvent. DES/AOT-SEDDS-F4 (containing 0.07% w/w DES/AOT) was composed of 50% Capmul 907P, 40% Cremophor RH40, and 10% Transcutol. The comparatively more hydrophilic formulation DES/AOT-SEDDS-F15 (containing 0.25% w/w DES/AOT) consisted of 20% Capmul 907P, 40% Acconon MC8-2, and 40% Tween 20. Both formulations were stable toward digestion by lipase and protected desmopressin toward a-chymotrypsin degradation. Moreover, DES/AOT-SEDDS-F4 also protected the peptide from thiol/disulfide exchange reactions with glutathione and was not cytotoxic at a concentration of 0.375% (w/w). Conclusion: DES/AOT-SEDDS-F4 protected desmopressin from in vitro glutathione and a-chymotrypsin degradation. DES/AOT-SEDDS-F4 was metabolically stable and nontoxic. Therefore, it could be considered as a potential delivery system for oral desmopressin administration.

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Evaluation of cytotoxicity of oils used in coenzyme Q10 Self-Emulsifying Drug Delivery Systems (SEDDS)

Cited by 60 publications

References 21 publications

Bioavailability Assessment of Vitamin A Self-Nanoemulsified Drug Delivery Systems in Rats: A Comparative Study

Bioavailability Assessment of Vitamin A Self-Nanoemulsified Drug Delivery Systems in Rats: A Comparative Study

A comparative study of a novel lipophilic phthalocyanine incorporated into nanoemulsion formulations: Photophysics, size, solubility and thermodynamic stability

Development andin vitroevaluation of an oral SEDDS for desmopressin

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