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Serratiopeptidase Niosomal Gel with Potential in Topical Delivery.

Shinde UA, Kanojiya SS - J Pharm (Cairo) (2014)

Bottom Line: The entrapment efficiency was found to be influenced by the molar ratio of Span 40 : cholesterol and concentration of SRP in noisome.Furthermore ex vivo skin permeation revealed that there was fourfold increase in a steady state flux when SRP was formulated in niosomes and a significant increase in the permeation of SRP, from SRP niosomal gel containing permeation enhancer.In vivo efficacy studies indicated that SRP niosomal gel had a comparable topical anti-inflammatory activity to that of dicolfenac gel.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, Bombay College of Pharmacy, Kalina, Santacruz (East), Mumbai 400098, India.

ABSTRACT
The objective of present study was to develop nonionic surfactant vesicles of proteolytic enzyme serratiopeptidase (SRP) by adapting reverse phase evaporation (REV) technique and to evaluate the viability of SRP niosomal gel in treating the topical inflammation. The feasibility of SRP niosomes by REV method using Span 40 and cholesterol has been successfully demonstrated in this investigation. The entrapment efficiency was found to be influenced by the molar ratio of Span 40 : cholesterol and concentration of SRP in noisome. The developed niosomes were characterized for morphology, particle size, and in vitro release. Niosomal gel was prepared by dispersing xanthan gum into optimized batch of SRP niosomes. Ex vivo permeation and in vivo anti-inflammatory efficacy of gel formulation were evaluated topically. SRP niosomes obtained were round in nanosize range. At Span 40 : cholesterol molar ratio 1 : 1 entrapment efficiency was maximum, that is, 54.82% ± 2.08, and showed consistent release pattern. Furthermore ex vivo skin permeation revealed that there was fourfold increase in a steady state flux when SRP was formulated in niosomes and a significant increase in the permeation of SRP, from SRP niosomal gel containing permeation enhancer. In vivo efficacy studies indicated that SRP niosomal gel had a comparable topical anti-inflammatory activity to that of dicolfenac gel.

No MeSH data available.


Related in: MedlinePlus

Cumulative amount of SRP permeated through rat skin.
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Related In: Results  -  Collection


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fig4: Cumulative amount of SRP permeated through rat skin.

Mentions: Niosomes are composed of nonionic surfactants, which are biocompatible and relatively nontoxic and themselves serve as excellent penetration enhancers [20]. Niosome formulation is expected to penetrate the stratum corneum and exist intact in the whole horny layer. Once it enters into the stratum corneum, niosomes may simultaneously alter both the lipid and the polar pathways. To evaluate skin penetration of SRP, ex vivo skin penetration studies were performed using Wistar rat skin. In this study the permeation data obtained from SRP niosomes and niosomal gel was compared with aqueous solution of SRP. Table 4 and Figure 4 show skin permeation of SRP niosomes and niosomal gel. The cumulative amount of SRP permeated from SRP aqueous solution was very low (i.e., 189.18 ± 1.27 μg/cm2) as compared to niosomal dispersion of SRP (i.e., 916.22 ± 0.64 μg/cm2); it could be because of high molecular weight of SRP, high water solubility, and low permeability. The mean flux of SRP from niosomal SRP dispersion was high (116.7 ± 2.15 μg/cm2 hr) with high permeability coefficient (0.306). The high mean flux (116.7 ± 2.15 μg/cm2 hr) in niosomal dispersion could be due to penetration enhancement effect of nonionic surfactants in vesicles. However, cumulative amount permeated through niosomal gel was low, that is, 96.45 ± 1.25 μg/cm2. SRP is a hydrophilic protein (proteolytic) enzyme and has high molecular weight of about 52 kDa; thereby, its skin permeation is poor and therefore permeation through skin becomes rate limiting step. Thus, in the case of peptides the permeation enhancement required is substantially greater due to their hydrophilicity and high molecular weight. Thus, to enhance SRP permeation through the rat skin combined strategies of niosomal gels formulated with penetration enhancers were studied. The study performed by Foldvari et al. showed that encapsulation of interferon (INF)-α in liposomes leads to increased deposition in the skin, but increased penetration of macromolecules through the skin has not been demonstrated [21]. Several penetration enhancement techniques such as chemical modification to form a conjugate with increased lipophilicity and encapsulation into hydrophobic carriers and incorporation of penetration enhancers which chemically or physically reduce the stratum corneum barrier have been developed to overcome the skin barrier and to facilitate the permeation of such high molecular peptides and proteins through the skin. Thus, to enhance SRP permeation through the rat skin combined strategies of niosomal gels formulated with penetration enhancers were studied. To evaluate the combined effect of the enhancers with non-onic surfactant vesicles on skin penetration of SRP, that is, to improve the ex vivo skin permeation, the SRP niosomal gels were prepared by incorporating 50% dimethylsulfoxide (DMSO). SRP niosomal xanthan gum gels with 50% DMSO showed 316.43 ± 1.5% cumulative release. In presence of penetration enhancer the values of the mean flux, permeability coefficient, and enhancement ratio were increased.


Serratiopeptidase Niosomal Gel with Potential in Topical Delivery.

Shinde UA, Kanojiya SS - J Pharm (Cairo) (2014)

Cumulative amount of SRP permeated through rat skin.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4590824&req=5

fig4: Cumulative amount of SRP permeated through rat skin.
Mentions: Niosomes are composed of nonionic surfactants, which are biocompatible and relatively nontoxic and themselves serve as excellent penetration enhancers [20]. Niosome formulation is expected to penetrate the stratum corneum and exist intact in the whole horny layer. Once it enters into the stratum corneum, niosomes may simultaneously alter both the lipid and the polar pathways. To evaluate skin penetration of SRP, ex vivo skin penetration studies were performed using Wistar rat skin. In this study the permeation data obtained from SRP niosomes and niosomal gel was compared with aqueous solution of SRP. Table 4 and Figure 4 show skin permeation of SRP niosomes and niosomal gel. The cumulative amount of SRP permeated from SRP aqueous solution was very low (i.e., 189.18 ± 1.27 μg/cm2) as compared to niosomal dispersion of SRP (i.e., 916.22 ± 0.64 μg/cm2); it could be because of high molecular weight of SRP, high water solubility, and low permeability. The mean flux of SRP from niosomal SRP dispersion was high (116.7 ± 2.15 μg/cm2 hr) with high permeability coefficient (0.306). The high mean flux (116.7 ± 2.15 μg/cm2 hr) in niosomal dispersion could be due to penetration enhancement effect of nonionic surfactants in vesicles. However, cumulative amount permeated through niosomal gel was low, that is, 96.45 ± 1.25 μg/cm2. SRP is a hydrophilic protein (proteolytic) enzyme and has high molecular weight of about 52 kDa; thereby, its skin permeation is poor and therefore permeation through skin becomes rate limiting step. Thus, in the case of peptides the permeation enhancement required is substantially greater due to their hydrophilicity and high molecular weight. Thus, to enhance SRP permeation through the rat skin combined strategies of niosomal gels formulated with penetration enhancers were studied. The study performed by Foldvari et al. showed that encapsulation of interferon (INF)-α in liposomes leads to increased deposition in the skin, but increased penetration of macromolecules through the skin has not been demonstrated [21]. Several penetration enhancement techniques such as chemical modification to form a conjugate with increased lipophilicity and encapsulation into hydrophobic carriers and incorporation of penetration enhancers which chemically or physically reduce the stratum corneum barrier have been developed to overcome the skin barrier and to facilitate the permeation of such high molecular peptides and proteins through the skin. Thus, to enhance SRP permeation through the rat skin combined strategies of niosomal gels formulated with penetration enhancers were studied. To evaluate the combined effect of the enhancers with non-onic surfactant vesicles on skin penetration of SRP, that is, to improve the ex vivo skin permeation, the SRP niosomal gels were prepared by incorporating 50% dimethylsulfoxide (DMSO). SRP niosomal xanthan gum gels with 50% DMSO showed 316.43 ± 1.5% cumulative release. In presence of penetration enhancer the values of the mean flux, permeability coefficient, and enhancement ratio were increased.

Bottom Line: The entrapment efficiency was found to be influenced by the molar ratio of Span 40 : cholesterol and concentration of SRP in noisome.Furthermore ex vivo skin permeation revealed that there was fourfold increase in a steady state flux when SRP was formulated in niosomes and a significant increase in the permeation of SRP, from SRP niosomal gel containing permeation enhancer.In vivo efficacy studies indicated that SRP niosomal gel had a comparable topical anti-inflammatory activity to that of dicolfenac gel.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, Bombay College of Pharmacy, Kalina, Santacruz (East), Mumbai 400098, India.

ABSTRACT
The objective of present study was to develop nonionic surfactant vesicles of proteolytic enzyme serratiopeptidase (SRP) by adapting reverse phase evaporation (REV) technique and to evaluate the viability of SRP niosomal gel in treating the topical inflammation. The feasibility of SRP niosomes by REV method using Span 40 and cholesterol has been successfully demonstrated in this investigation. The entrapment efficiency was found to be influenced by the molar ratio of Span 40 : cholesterol and concentration of SRP in noisome. The developed niosomes were characterized for morphology, particle size, and in vitro release. Niosomal gel was prepared by dispersing xanthan gum into optimized batch of SRP niosomes. Ex vivo permeation and in vivo anti-inflammatory efficacy of gel formulation were evaluated topically. SRP niosomes obtained were round in nanosize range. At Span 40 : cholesterol molar ratio 1 : 1 entrapment efficiency was maximum, that is, 54.82% ± 2.08, and showed consistent release pattern. Furthermore ex vivo skin permeation revealed that there was fourfold increase in a steady state flux when SRP was formulated in niosomes and a significant increase in the permeation of SRP, from SRP niosomal gel containing permeation enhancer. In vivo efficacy studies indicated that SRP niosomal gel had a comparable topical anti-inflammatory activity to that of dicolfenac gel.

No MeSH data available.


Related in: MedlinePlus