Description:FIELD OF THE INVENTION
[0001] The present invention generally relates to pharmaceutical composition. Specifically, the present invention relates to a nanosponge composition comprising of bergenin and a pharmaceutically acceptable excipients. The present invention also relates to a process of preparation of the nanosponge composition and its use thereof.

BACKGROUND OF THE INVENTION
[0002] Background description includes information that may be useful in understanding the present invention. It is not an admission that any of the information provided herein is prior art or relevant to the presently claimed invention, or that any publication specifically or implicitly referenced is prior art.
[0003] The varieties of biological activities starting from antioxidant to anticancer have been reported for a phytocompound, Bergenin in literature. According to Biopharmaceutics Classification System (BCS) scheme, bergenin has been classified as class IV compound. Bergenin has neither sufficient solubility nor permeability for complete absorption and therefore offering poor oral bioavailability.
[0004] As a result of rapid advances in nanotechnology, nanosponges are an innovative drug delivery system that has recently emerged for precise and targeted drug delivery. Nanosponges are very small, microscopic, and tiny mesh-like structures with a size less than 1µm. It consists of a number of cavities that can be filled with medications/drugs.
[0005] IN202011051492 discloses nanosponge formulation of felodipine and method of preparation thereof containing disperse phase and aqueous phase, wherein the disperse phase is added to an aqueous phase then the mixture was stirred for 1-2 hr to form nanosponge formulation.
[0006] Polym. Chem., 2014, 11(5), 3551-3554 discloses nanosponge formulation of BCS class IV drug. The cited document also disclose that nanosponges for oral administration of BSC IV class drugs to afford high solubilization, high permeability and a fully adjustable release profile of the therapeutic.
[0007] There is, therefore, a need to develop a nanosponge composition comprising of Bergenin which has improved solubility, stability and bioavailability and is safe.

OBJECTS OF THE INVENTION
[0008] An object of the present invention is to provide a nanosponge composition comprising of Bergenin.
[0009] Another object of the present invention is to provide a nanosponge composition comprising of Bergenin that has improved solubility, stability and bioavailability.
[0010] Another object of the present invention is to provide a process of preparation of a nanosponge composition comprising of Bergenin.

SUMMARY OF THE INVENTION
[0011] The present invention generally relates to pharmaceutical composition. Specifically, the present invention relates to a nanosponge composition comprising of bergenin and a pharmaceutically acceptable excipients. The present invention also relates to a process of preparation of the nanosponge composition and its use thereof.
[0012] In one aspect, the present invention relates to a nanosponge composition comprising of:
(a) Bergenin;
(b) resin; and
(c) optionally pharmaceutically acceptable excipients.
[0013] In another embodiment of the present invention, the resin is mastic gum.
[0014] In another embodiment of the present invention, the pharmaceutically acceptable excipients are selected from solvent, polyvinyl alcohol or mixture thereof.
[0015] In another embodiment of the present invention, the solvent is dichloromethane, chloroform, ethyl acetate or a mixture thereof.
[0016] In another aspect, the present invention relates to the composition comprising of:
(a) Bergenin;
(b) mastic gum;
(c) polyvinyl alcohol;
(d) dichloromethane; and
(e) water as required.
[0017] In an embodiment of the present invention, the Bergenin is present in an amount ranges from about 0.06% to 0.1 % weight of the composition.
[0018] In another embodiment of the present invention, the mastic gum is present in an amount ranges from about 0.1% to about 0.2 % by weight of the composition.
[0019] In another embodiment of the present invention, wherein the polyvinyl alcohol is present in an amount of about 1% to about 1.5 % by weight of the composition.
[0020] In another embodiment of the present invention, the composition is in the form of cream, gel, solution, lotion or foam.
[0021] In yet another aspect, the present invention relates to a process for preparation of nanosponge composition comprising the steps of:
(a) preparing an organic phase comprising of Bergenin and mastic gum in a dichloromethane;
(b) preparing an aqueous phase comprising of polyvinyl alcohol in water; and
(c) mixing the organic phase with the aqueous phase under stirring for a period of 1-2 hours at room temperature to obtain nanosponge formulation.
[0022] Various objects, features, aspects and advantages of the inventive subject matter will become more apparent from the following detailed description of preferred embodiments.
BRIEF DESCRIPTION OF THE FIGURES
[0023] Figure 1 shows the image of the bergenin embedded nanosponge of the present invention.
[0024] Figure 2 depicts the Zeta potential value of the bergenin embedded nanosponge of the present invention.

DETAILED DESCRIPTION OF THE INVENTION
[0025] The following is a detailed description of embodiments of the disclosure. The embodiments are in such detail as to clearly communicate the disclosure. However, the amount of detail offered is not intended to limit the anticipated variations of embodiments; on the contrary, the intention is to cover all modifications, equivalents, and alternatives falling within the spirit and scope of the present disclosure as defined by the appended claims.
[0026] Unless the context requires otherwise, throughout the specification which follow, the word “comprise” and variations thereof, such as, “comprises” and “comprising” are to be construed in an open, inclusive sense that is as “including, but not limited to.”
[0027] Reference throughout this specification to “one embodiment” or “an embodiment” means that a particular feature, structure or characteristic described in connection with the embodiment is included in at least one embodiment. Thus, the appearances of the phrases “in one embodiment” or “in an embodiment” in various places throughout this specification are not necessarily all referring to the same embodiment. Furthermore, the particular features, structures, or characteristics may be combined in any suitable manner in one or more embodiments.
[0028] As used in this specification and the appended claims, the singular forms “a,” “an,” and “the” include plural referents unless the content clearly dictates otherwise. It should also be noted that the term “or” is generally employed in its sense including “and/or” unless the content clearly dictates otherwise.
[0029] In some embodiments, the numbers expressing quantities of ingredients, properties such as concentration, reaction conditions, and so forth, used to describe and claim certain embodiments of the invention are to be understood as being modified in some instances by the term “about.” Accordingly, in some embodiments, the numerical parameters set forth in the written description are approximations that can vary depending upon the desired properties sought to be obtained by a particular embodiment. In some embodiments, the numerical parameters should be construed in light of the number of reported significant digits and by applying ordinary rounding techniques. Notwithstanding that the numerical ranges and parameters setting forth the broad scope of some embodiments of the invention are approximations, the numerical values set forth in the specific examples are reported as precisely as practicable.
[0030] The recitation of ranges of values herein is merely intended to serve as a shorthand method of referring individually to each separate value falling within the range. Unless otherwise indicated herein, each individual value is incorporated into the specification as if it were individually recited herein.
[0031] All processes described herein can be performed in any suitable order unless otherwise indicated herein or otherwise clearly contradicted by context. The use of any and all examples, or exemplary language (e.g. “such as”) provided with respect to certain embodiments herein is intended merely to better illuminate the invention and does not pose a limitation on the scope of the invention otherwise claimed. No language in the specification should be construed as indicating any non-claimed element essential to the practice of the invention.
[0032] The headings and abstract of the invention provided herein are for convenience only and do not interpret the scope or meaning of the embodiments.
[0033] The following discussion provides many example embodiments of the inventive subject matter. Although each embodiment represents a single combination of inventive elements, the inventive subject matter is considered to include all possible combinations of the disclosed elements. Thus if one embodiment comprises elements A, B, and C, and a second embodiment comprises elements B and D, then the inventive subject matter is also considered to include other remaining combinations of A, B, C, or D, even if not explicitly disclosed.
[0034] All publications herein are incorporated by reference to the same extent as if each individual publication or patent application were specifically and individually indicated to be incorporated by reference. Where a definition or use of a term in an incorporated reference is inconsistent or contrary to the definition of that term provided herein, the definition of that term provided herein applies and the definition of that term in the reference does not apply.
[0035] Groupings of alternative elements or embodiments of the invention disclosed herein are not to be construed as limitations. Each group member can be referred to and claimed individually or in any combination with other members of the group or other elements found herein. One or more members of a group can be included in, or deleted from, a group for reasons of convenience and/or patentability. When any such inclusion or deletion occurs, the specification is herein deemed to contain the group as modified thus fulfilling the written description that follows, and the embodiments described herein, is provided by way of illustration of an example, or examples, of particular embodiments of the principles and aspects of the present disclosure. These examples are provided for the purposes of explanation, and not of limitation, of those principles and of the disclosure.
[0036] It should also be appreciated that the present invention can be implementedin numerous ways, including as a system, a method or a device. In this specification, these implementations, or any other form that the invention may take, may be referred to as processes. In general, the order of the steps of the disclosed processes may be altered within the scope of the invention.
[0037] Various terms as used herein are shown below. To the extent a term used in a claim is not defined below, it should be given the broadest definition persons in the pertinent art have given that term as reflected in printed publications and issued patents at the time of filing.
[0038] The term "about" as used herein refers to a defined range of the value by plus or minus 10 %.For example, about 2 % means 1.8 % to 2.2 %, about 5 % means 4.5 % to 5.5 %, about 10 % means 9 % to 11 % and about 40 % means 36 % to 44 %.
[0039] In a general embodiment, present invention generally relates to pharmaceutical composition. Specifically, the present invention relates to a nanosponge composition comprising of bergenin and a pharmaceutically acceptable excipients. The present invention also relates to a process of preparation of the nanosponge composition and its use thereof.
[0040] In an embodiment, the present invention relates to nanosponge composition comprising of:
(a) Bergenin;
(b) mastic gum;
(c) polyvinyl alcohol;
(d) solvent; and
(e) water as required.
[0041] In another embodiment of the present invention, the Bergenin and mastic gum is present in a ration ranges from 1:2 to 1:5 or vice versa.
[0042] In another aspect, the present invention relates to a nanosponge composition comprising of:
(a) about 0.06% to about 0.1% of Bergenin by weight of the composition;
(b) about 0.1% to about 0.2% of mastic gum by weight of the composition;
(c) about 1% to about 1.5% of polyvinyl alcohol by weight of the composition;
(e) water q.s.
[0043] In another embodiment of the present invention, the solvent is selected from dichloromethane, chloroform, dimethyl sulfoxide, methanol etc.
[0044] In another embodiment, the Bergenin is present in an amount of 0.05%, 0.1%, 0.2%, 0.5% by weight of the composition. Most preferably, in an amount of 0.06 % to 0.1% by weight of the composition.
[0045] In another embodiment, the mastic gum is present in an amount of 0.1%, 0.2%, 0.3%, 0.5% by weight of the composition. Most preferably, in an amount of 0.1% to about 0.2% by weight of the composition.
[0046] In another embodiment, the polyvinyl alcohol is present in an amount 0.5%, 1%, 1.5%, 2% and 2.5% by weight of the composition. Most preferably, in an amount of 1% to 1.5% by weight of the composition.
[0047] In an embodiment, the nanosponge composition of the present invention is non-toxic and stable at higher temperature compared to other nano formulation.
[0048] In another embodiment, the nanosponge composition of the present invention shows improved solubility, stability and bioavailability.
[0049] According to the present invention, the nanosponge composition can be compatible with different routes of administration like oral, topical and intravenous.
[0050] The present invention provides a nanogel formulation comprising of Bergenin. The formulation is ideal oil in water formulation with good consistency, smooth and shining texture, and good stability.
[0051] In yet another embodiment, the present invention relates to a process for preparation of nanosponge composition comprising the steps of:
(a) preparing an organic phase comprising of Bergenin and polymer in a solvent;
(b) preparing an aqueous phase comprising of polyvinyl alcohol in water; and
(c) mixing the organic phase with the aqueous phase under stirring for a period of 1-2 hours to obtain nanosponge formulation.
[0052] In yet another embodiment, the present invention relates to a process for preparation of nanosponge composition comprising the steps of:
(a) preparing an organic phase comprising of Bergenin and mastic gum in a dichloromethane;
(b) preparing an aqueous phase comprising of polyvinyl alcohol in water; and
(c) mixing the organic phase with the aqueous phase under stirring for a period of 1-2 hours at room temperature to obtain nanosponge formulation.
[0053] In another embodiment, the pharmaceutical composition of the present invention can be useful in the treatment of fungal, viral, bacterial and cancer diseases.
[0054] While the foregoing describes various embodiments of the disclosure, other and further embodiments of the disclosure may be devised without departing from the basic scope thereof. The scope of the invention is determined by the claims that follow. The invention is not limited to the described embodiments, versions or examples, which are included to enable a person having ordinary skill in the art to make and use the invention when combined with information and knowledge available to the person having ordinary skill in the art.
EXAMPLES
[0055] The present invention is further explained in the form of following examples. However, it is to be understood that the following examples are merely illustrative and are not to be taken as limitations upon the scope of the invention.
Example 1: Preparation of nanosponge formulation
Essential Ingredients:
Sr. No. Name of Ingredients Weight (g)
1. Bergenin 0.1
2. Mastic Gum 0.2
3. Poly vinyl alcohol (PVA) 2
4. Dichloromethane (DCM) 20 ml
5. Water 150 ml

[0056] The formulation components listed in the table above were used in the preparation of nanosponge formulation.
Step – 1: Preparation of Organic Phase
Bergenin (0.1 g) and mastic gum (0.2 g) were added to dichloromethane (20 ml) under stirring to obtain an organic phase.
Step – 2: Preparation of aqueous Phase
Poly vinyl alcohol (20 ml) was added to water (150 ml) under stirring to obtain an aqueous phase.
Step -3: Preparation of Nanosponge
The organic phase was added to aqueous phase under stirring. The stirring was continued for 2 hours at room temperature to obtain the nanosponge. Figure 1 shows the image of bergenin embedded nanosponge. Figure 2 shows the Zeta potential value.
Characterization of Bergenin loaded Nanosponges
S. No Parameters Values
1. Percentage Yield 87.2%
2. Drug entrapment efficiency 99.89%
3. Particle size 112±0.01 nm
4 Zeta Potential -0.114mV

Solubility of Bergenin and Bergenin Nanosponges in water:
S. No Drug Soluble Sparing Soluble Insoluble
1. Bergenin ?
2. Bergenin nano sponges ?

[0057] A skilled artisan will appreciate that the quantity and type of each ingredient can be used in different combinations or singly. All such variations and combinations would be falling within the scope of present disclosure

[0058] The foregoing examples are merely illustrative and are not to be taken as limitations upon the scope of the invention. Various changes and modifications to the disclosed embodiments will be apparent to those skilled in the art. Such changes and modifications may be made without departing from the scope of the invention.

We Claims:

1. A nanosponge composition comprising of:
(a) Bergenin,
(b) resin; and
(c) optionally pharmaceutically acceptable excipients.
2. The nanosponge composition as claimed in claim 1, wherein the resin is mastic gum.
3. The nanosponge composition as claimed in claim 1, wherein the pharmaceutically acceptable excipients are selected from solvent, polyvinyl alcohol or mixture thereof.
4. The nanosponge composition as claimed in claim 1, wherein the solvent is dichloromethane, chloroform, ethyl acetate or a mixture thereof.
5. The nanosponge composition as claimed in claim 1, wherein the composition comprises:
(a) Bergenin;
(b) mastic gum;
(c) polyvinyl alcohol;
(d) dichloromethane; and
(e) water as required.
6. The nanosponge composition as claimed in claim 5, wherein the Bergenin is present in an amount ranges from about 0.06% to about 0.1% by weight of the composition.
7. The nanosponge composition as claimed in claim 5, wherein the mastic gum is present in an amount ranges from about 0.1% to about 0.2% by weight of the composition.
8. The nanosponge composition as claimed in claim 5, wherein the polyvinyl alcohol is present in an amount of about 1% to about 1.5 % by weight of the composition.
9. The nanosponge composition as claimed in any one of the claims 1 to 8, wherein the composition is in the form of cream, gel, solution, lotion or foam.
10. A process for preparation of nanosponge composition comprising the steps of:
(a) preparing an organic phase comprising of Bergenin and mastic gum in a dichloromethane;
(b) preparing an aqueous phase comprising of polyvinyl alcohol in water; and
(c) mixing the organic phase with the aqueous phase under stirring for a period of 1-2 hours at room temperature to obtain nanosponge formulation.