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Development and optimization of polymeric self-emulsifying nanocapsules for localized drug delivery: design of experiment approach.

Wadhwa J, Asthana A, Gupta S, Shilkari Asthana G, Singh R - ScientificWorldJournal (2014)

Bottom Line: Polymeric nanocapsules with an average diameter of 100-180 nm and an encapsulation efficiency of 64.85±0.12% were obtained.Roentgenography study confirms the localized presence of carrier (0-2 h in upper GIT; 2-4 h in small intestine; and 4-24 h in the lower intestine).The present study demonstrates systematic development of polymeric self-emulsifying nanocapsule formulation of curcumin for localized targeting in colon.

View Article: PubMed Central - PubMed

Affiliation: MM College of Pharmacy, MM University, Mullana, Ambala 133207, India.

ABSTRACT
The purpose of the present study was to formulate polymeric self-emulsifying curcumin nanocapsules with high encapsulation efficiency, good emulsification ability, and optimal globule size for localized targeting in the colon. Formulations were prepared using modified quasiemulsion solvent diffusion method. Concentration of formulation variables, namely, X1 (oil), X2 (polymeric emulsifier), and X3 (adsorbent), was optimized by design of experiments using Box-Behnken design, for its impact on mean globule size (Y1) and encapsulation efficiency (Y2) of the formulation. Polymeric nanocapsules with an average diameter of 100-180 nm and an encapsulation efficiency of 64.85±0.12% were obtained. In vitro studies revealed that formulations released the drug after 5 h lag time corresponding to the time to reach the colonic region. Pronounced localized action was inferred from the plasma concentration profile (C max 200 ng/mL) that depicts limited systemic absorption. Roentgenography study confirms the localized presence of carrier (0-2 h in upper GIT; 2-4 h in small intestine; and 4-24 h in the lower intestine). Optimized formulation showed significantly higher cytotoxicity (IC50 value 20.32 μM) in HT 29 colonic cancer cell line. The present study demonstrates systematic development of polymeric self-emulsifying nanocapsule formulation of curcumin for localized targeting in colon.

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Overlay of XRPD pattern of A. free CUR; B. HPMCAS-HF; C. physical mixture; and D. optimized formulation (P5).
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fig8: Overlay of XRPD pattern of A. free CUR; B. HPMCAS-HF; C. physical mixture; and D. optimized formulation (P5).

Mentions: XRPD of CUR describes its crystalline nature. Majority of peaks for CUR occurred at 16.97, 25.20, 16.92, 24.19, 27.02, 25.15, 24.24, 26.97, 17.02, 27.07, 25.30, 23.03, 24.14, 26.92, 22.98, and 28.59° 2θ, whereas peak with highest intensity was observed at 25.25 (Figure 8).


Development and optimization of polymeric self-emulsifying nanocapsules for localized drug delivery: design of experiment approach.

Wadhwa J, Asthana A, Gupta S, Shilkari Asthana G, Singh R - ScientificWorldJournal (2014)

Overlay of XRPD pattern of A. free CUR; B. HPMCAS-HF; C. physical mixture; and D. optimized formulation (P5).
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4265377&req=5

fig8: Overlay of XRPD pattern of A. free CUR; B. HPMCAS-HF; C. physical mixture; and D. optimized formulation (P5).
Mentions: XRPD of CUR describes its crystalline nature. Majority of peaks for CUR occurred at 16.97, 25.20, 16.92, 24.19, 27.02, 25.15, 24.24, 26.97, 17.02, 27.07, 25.30, 23.03, 24.14, 26.92, 22.98, and 28.59° 2θ, whereas peak with highest intensity was observed at 25.25 (Figure 8).

Bottom Line: Polymeric nanocapsules with an average diameter of 100-180 nm and an encapsulation efficiency of 64.85±0.12% were obtained.Roentgenography study confirms the localized presence of carrier (0-2 h in upper GIT; 2-4 h in small intestine; and 4-24 h in the lower intestine).The present study demonstrates systematic development of polymeric self-emulsifying nanocapsule formulation of curcumin for localized targeting in colon.

View Article: PubMed Central - PubMed

Affiliation: MM College of Pharmacy, MM University, Mullana, Ambala 133207, India.

ABSTRACT
The purpose of the present study was to formulate polymeric self-emulsifying curcumin nanocapsules with high encapsulation efficiency, good emulsification ability, and optimal globule size for localized targeting in the colon. Formulations were prepared using modified quasiemulsion solvent diffusion method. Concentration of formulation variables, namely, X1 (oil), X2 (polymeric emulsifier), and X3 (adsorbent), was optimized by design of experiments using Box-Behnken design, for its impact on mean globule size (Y1) and encapsulation efficiency (Y2) of the formulation. Polymeric nanocapsules with an average diameter of 100-180 nm and an encapsulation efficiency of 64.85±0.12% were obtained. In vitro studies revealed that formulations released the drug after 5 h lag time corresponding to the time to reach the colonic region. Pronounced localized action was inferred from the plasma concentration profile (C max 200 ng/mL) that depicts limited systemic absorption. Roentgenography study confirms the localized presence of carrier (0-2 h in upper GIT; 2-4 h in small intestine; and 4-24 h in the lower intestine). Optimized formulation showed significantly higher cytotoxicity (IC50 value 20.32 μM) in HT 29 colonic cancer cell line. The present study demonstrates systematic development of polymeric self-emulsifying nanocapsule formulation of curcumin for localized targeting in colon.

Show MeSH
Related in: MedlinePlus