Ex-vivo absorption study of a nanoparticle based novel drug delivery system of vitamin D3 (Arachitol Nano™) using everted intestinal sac technique

Bothiraja, C.; Pawar, Atmaram; Deshpande, G. D.

doi:10.1007/s40005-016-0235-2

Cited by 21 publications

(9 citation statements)

References 23 publications

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“…46 To provide a sink condition for permeation and taking into consideration the effect of solvent on the intestine viability, a mixture of Krebs-Ringer phosphate buffer saline, pH 7.4, and isopropyl alcohol in the ratio of 7:3 (v/v) was chosen in accordance with previous reports. 47 It was noticed that all permeated drug was measured as rhein, which agreed with previous reports that DCN is completely converted into rhein before reaching the circulation. 48 As shown in Figure 5, the cumulative amounts permeated after 120 minutes were 450.48±10.51, 108.28±1.06, and 97.83±6.53 µg for DNS-F7, CS-DNS-F10, and DCN suspension, respectively.…”

Section: Ex Vivo Permeationsupporting

confidence: 90%

Chitosan-coated diacerein nanosuspensions as a platform for enhancing bioavailability and lowering side effects: preparation, characterization, and ex vivo/in vivo evaluation

Allam¹,

Hamdallah²,

Abdallah³

2017

IJN

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Nanodrug delivery systems have been widely reviewed for their use in several drug formulations to improve bioavailability, sustain effect, and decrease side effects of many candidate drugs. The objective of this study was to evaluate the potential of chitosan (CS)-coated nanosuspensions to enhance bioavailability and reduce the diarrheal side effect of diacerein (DCN) after oral administration. DCN nanosuspensions (DNS) were prepared by sonoprecipitation technique using different stabilizers at three different concentrations. The selected DNS with optimum particle size (PS), polydispersity index (PDI), and Zeta potential (ZP) was coated with three different concentrations of CS-coated DNS (CS-DNS) and screened. In vitro dissolution was performed for the selected lyophilized formulae and compared with DCN powder in addition to the assessment of drug crystallinity via scanning electron microscopy, X-ray powder diffraction, and differential scanning calorimetry. Ex vivo drug permeability using noneverted rat intestine, intraluminal content, and mucoadhesion evaluation was studied for nominated formulae in comparison to DCN suspension. Moreover, in vivo study, pharmacokinetic parameters, and evaluation of diarrheal potential were conducted after oral administration of selected formulae. Polyvinyl pyrrolidone (PVP)-stabilized DNS showed a significant increase ( P ≤0.05) in PS and PDI as the stabilizer concentration increased. PVP-stabilized DNS with the lowest CS concentration was protected from aggregation by lyophilization with mannitol. A remarked enhancement in dissolution parameters was observed in the nanocrystals’ formulae. Morphological examination and X-ray diffraction confirmed drug crystallinity. The intermediate permeation parameters of CS-DNS-F10, lowest rhein-to-DCN ratio in intraluminal content along with the highest percentage of mucoadhesive, could serve as a sustaining profile of coated formula. CS-DNS-F10 showed a significantly higher C max of 0.74±0.15 µg/mL at a delayed T max of 3.60±0.55 hours with a relative bioavailability of 172.1% compared to DCN suspension. CS-coated nanosuspensions could serve as promising revenue to enhance bioavailability and reduce the diarrheal side effect of DCN after oral administration.

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Section: Ex Vivo Permeationsupporting

confidence: 90%

Chitosan-coated diacerein nanosuspensions as a platform for enhancing bioavailability and lowering side effects: preparation, characterization, and ex vivo/in vivo evaluation

Allam¹,

Hamdallah²,

Abdallah³

2017

IJN

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“…19,20 The improvement in absorption could be because nanoparticles reduce the necessity of lipids in the absorption, provide protection against harsh environment of the gastrointestinal tract and possibly enhance transmucosal transport. [19][20][21][22] Other researchers have also suggested that nanoparticles of vitamin D 3 may also enhance important properties of vitamin D supplements, like therapeutic efficacy, photo-stability and biodegradation. 19,20,22,23. Higher body fat percentage or higher BMI have been associated with smaller increases in 25 (OH) D concentrations in response to vitamin D supplementation.…”

Section: Discussionmentioning

confidence: 99%

“…This study also showed that nano particle based vitamin D absorbed through various part of rat small intestine like duodenum, jejunum, and ileum. 19 Until today no study on nano particle based vitamin D formulation in patients of vitamin D deficiencies is performed Hence, this study was planned to evaluate the efficacy of nanoparticle based vitamin D formulation in correcting the vitamin D levels after a weekly therapy for 8 weeks.…”

Section: Introductionmentioning

confidence: 99%

Evaluation of efficacy of a nanoparticle based vitamin D formulation in correction of vitamin D levels in patients with documented deficiency or insufficiency of vitamin D

Manek¹

2017

Int J Res Orthop

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INTRODUCTIONVitamin D deficiency has been proposed to contribute to the development of various diseases.1 It has been estimated that one billion people worldwide have Vitamin D deficiency. 2 In India more than 90% of apparently healthy Indians have subnormal 25(OH) D levels. [3][4][5][6] The endocrine society suggests that serum levels of 25 [OH] D less than 20 ng/ml as deficiency and levels between 21-29 ng/mL as insufficiency, while levels of 25[OH] D above 30 ng/mL are optimum levels of the vitamin. 7Sunlight is known to be the primary source of vitamin D and its production in the skin depends on exposure to sunshine, latitude, skin-covering clothes, the use of sunscreen lotions and skin pigmentation in healthy individuals. The status of vitamin D depends on the Patients who have received treatment for at least 4 weeks' period (n=38), the improvement (serum 25[OH] D >30 ng/ml) was seen in 84.2% patients (n=32) at the end of 4 weeks itself. There is significant increased (<0.0001) in the physical component scores of the SF-12 QOL questionnaire after 8 weeks of therapy. Conclusions: Nanoparticle based formulation of vitamin D 3 is effective and safe in correction of vitamin D levels in patients with documented deficiency or insufficiency of vitamin D. Also the safety and tolerability is well accepted and reported good to excellent by patients and physician.

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“…The efficiency of oral absorption of conventional Vitamin D3 is approximately 50%. 11 In general, the availability for absorption of a drug is more in oral solutions comparing to the capsule and tablet respectively. 12 Bioavailability of vitamin D can be increased by nanotechnology in an effective way.…”

Section: Introductionmentioning

confidence: 99%

Relative oral bioavailability of three formulations of vitamin D3: An open-label, three-treatment study

Nandgaye¹,

Samant²,

Kadam³

et al. 2018

Int J Basic Clin Pharmacol

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Background: Supplementation of vitamin D2 or vitamin D3 is recommended for vitamin D deficiency. Weekly supplementation of 60,000 IU of vitamin D3 increases serum 25(OH) D to optimal values. Various marketed forms of vitamin D3 include tablets, capsule, granules and oral solution. The main objective of this study is to compare the relative bioavailability of vitamin D3 oral solution with vitamin D3 tablet and capsule.Methods: This is an open-label, randomized, single-dose, three-treatment study to compare the relative bioavailability of vitamin D3 oral solution with capsule and tablet. Subjects (n=70) were supplemented with single dose of one of these formulations and their blood sample were assessed for Cmax, AUC0-28d and Tmax.Results: The logarithmic transformed data of pharmacokinetic parameters were analyzed for 90% Confidence Intervals (CI) using ANOVA. The mean (90% CI) values of vitamin D3 oral solution against tablet for the ratio of Cmax and AUC0-28d were 113.00 (105.32-121.23) and 105.54 (97.95-113.72) respectively. The mean (90% CI) values of vitamin D3 oral solution against capsule for the ratio of Cmax and AUC0-28d were 115.02 (106.38 - 124.37) and 112.33 (104.44 - 120.81) respectively. These values were within the bioequivalence range of 80-125%.Conclusions: It is concluded that vitamin D3 Oral Solution formulated with nanotechnology is bioequivalent to vitamin D3 tablet and capsule. However, oral solution of vitamin D3 shows higher Cmax and AUC when compared to tablet and capsule formulations.

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Ex-vivo absorption study of a nanoparticle based novel drug delivery system of vitamin D3 (Arachitol Nano™) using everted intestinal sac technique

Cited by 21 publications

References 23 publications

Chitosan-coated diacerein nanosuspensions as a platform for enhancing bioavailability and lowering side effects: preparation, characterization, and ex vivo/in vivo evaluation

Chitosan-coated diacerein nanosuspensions as a platform for enhancing bioavailability and lowering side effects: preparation, characterization, and ex vivo/in vivo evaluation

Evaluation of efficacy of a nanoparticle based vitamin D formulation in correction of vitamin D levels in patients with documented deficiency or insufficiency of vitamin D

Relative oral bioavailability of three formulations of vitamin D3: An open-label, three-treatment study

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