INTRODUCTION:

For almost fifty years, the idea of sophisticated drug delivery systems, particularly those that provide a controlled and prolonged action of the drug to the desired area of effect, has been very appealing. However, drug delivery systems were only thought of as a way to get the drug into the patient's body before better alternative techniques were developed.¹ The introduction of time release coating to tablets or solid medicine particles to cover up their unpalatable taste or make them more pleasant marked the beginning of the actual practice of controlled release. The production of micro speres has been studied using a variety of materials, both biodegradable and non-biodegradable.² These materials include modified natural compounds as well as polymers of synthetic and natural origin. Methyl methacrylate, acrolein, lactide, glycoside and their copolymers, ethylene vinyl acetate copolymer, and polyanhydrides are examples of synthetic polymers used as carrier materials. The natural polymers utilized for this purpose are collagen, carrageenan, albumin, gelatine, and Strach.³

Micro encapsulation, in which a polymer component is applied to a drug material, is a popular technique for regulating the rate of drug release. As a result, the process becomes impervious to toxicity and safety risks and lowers production costs, making the methods economically, environmentally, and reproducibly viable on an industrial scale.⁴ Researchers have looked at a variety of natural, semi-synthetic, and synthetic polymer materials. However, the synthetic polymers have demonstrated some limitations, and the mix of natural and synthetic polymers is complex and raises formulation costs.

Phyto phenols are significant food-based bioactive compounds that are mostly found in a variety of natural sources. One of the most important natural phenols among them is sesamol, which is present in Piper cubeba, sesame seeds, and other plants. Sesame oil is a powerful cardioprotective functional food, according to several research. Although there isn't a single, succinct study of the benefit of sesamol in sesame oil for CVD, there have been papers on the topic in the literature. Sesamol's chemical name is methylenedioxyphenol, or MDP.⁵

MATERIAL AND METHOD:

Sesamol was obtained from Yucca Enterprises, Mumbai India. Sodium alginate, chitosan, calcium chloride, disodium hydrogen phosphate potassium di hydrogen phosphate was purchased from oxford lab Mumbai.

Methods of Preparation:

The microspheres were created using the emulsion solvent evaporation method. By boiling it to between 40 and 50 degrees Celsius, sodium alginate was dissolved in an adequate volume of water. The aforesaid solution was then supplemented with the designated amount of the polymer (chitosan). Following the polymer's dissolution, the medication (Sesamol) was introduced and mixed throughout the polymeric solution while being constantly stirred for two hours.

As a cross-linking agent, a 5% calcium chloride solution in water was made in the meantime and put on the magnetic stirrer. Using needle 24 and constant stirring at 50 rpm, the drug and polymer mixture was poured into the syringe and added drop by drop into the calcium chloride solution. For two hours, the produced microspheres were left to cure in the calcium chloride solution. The produced microspheres were then properly kept after being filtered through Whatman filter paper and dried in a hot air oven set to 50 degrees Celsius.

Table 1. Formulation of Floating Microspheres of Sesamol

Batch	Drug (mg)	Sodium alginate (g)	Chitosan (g)	Calcium chloride (%)	Solvent
F1	100	1	0.5	5	30
F2	100	1	0.75	5	30
F3	100	1	1	5	30
F4	100	1	1.25	5	30
F5	100	1	1.50	5	30
F6	100	1	1.75	5	30

EVALUATION PARAMETERS:

· Calibration curve: The calibration curve was created for a range of 10–50 µg/mL, and the maximum absorbance of sesamol in methanol was determined to be 295 nm. The resulting curve was plotted with its absorbance on the y axis and sesamol on the x axis.⁶

· Compatibility study: With an FT-IR spectrophotometer, drug excipients compatibility was investigated prior to the development of floating microspheres^.7

· Micrometrics characteristics: The bulk density at the angle of repose, the tap density, the compressibility index, and the Hausner’s ratio were used to describe the microspheres.⁸

· Particles size: The size of particles was determined by a microsphere.

· Percentage yield: Calculating the % yield. Microspheres that had been completely

Dried were gathered and precisely weighed. The yield % was determined.⁹

Mass of the dried microspheres obtained

% yield = ----------------------------------------------* 100

Total Weight of drug and polymer

· Invitro drug release: Using a paddle-style dissolving test equipment, the in vitro release of sesamol from the microspheres was measured in phosphate buffer at pH 6.8. Microspheres containing 100 mg of the medication were taken, placed in capsules, and suspended in a dissolving media that was kept at 37 ± 0.5°C and 50 rpm. For the next six hours, 5 mL of the sample was taken out at various intervals and replaced with the same volume of fresh medium. After passing through Whatman filter paper, the samples were examined by a UV spectrophotometer at 295 nm to determine the amount of medication released.¹⁰

RESULT AND DISCUSSION:

Determination of λ max. The absorption maximum of sesamol in methanol was found to be 295 nm and the calibration curve was prepared for a range of 10-50 µg/mL.

Table 2. Concentration and absorbance for Sesamol

Sr. no.	Concentration (µg/mL)	Absorbance
1.	10	0.177
2.	20	0.350
3.	30	0.521
4.	40	0.701
5.	50	0.856

Fig. 1. Calibration curve of sesamol

Table 3. Micrometric analysis of made-up floating microspheres

Batch No.	Angel of Repose	Bulk Density	Tapped density	Hausner Ratio	Carr’s Index
F1	29.27	0.439	0.463	1.096	8.829
F2	27.70	0.445	0.465	1.139	12.258
F3	27.92	0.476	0.481	1.093	8.571
F4	26.10	0.479	0.487	1.057	5.405
F5	24.70	0.483	0.495	1.068	6.430
F6	25.64	0.488	0.503	1.122	10.874

Table 4. Percentage yield and particle size of microspheres

Batch	Yield (%)	Particle size (µm)	Drug content (%)
F1	56.4	33.86 ± 17.25	74.42
F2	59.8	30.63 ± 17.82	79.15
F3	74.2	33.37 ± 15.59	83.34
F4	74.4	29.88 ± 18.14	89.71
F5	73.9	34.61 ± 12.14	79.33
F6	74.1	35.36 ± 16.37	67.45

Table 5. Invitro drug release of Formulation

Time (h)	% Drug release
Time (h)	F1	F2	F3	F4	F5	F6
0	0	0	0	0	0	0
1	40.31	39.56	33.22	23.34	37.98	30.17
2	51.87	50.18	46.7	43.01	52.49	41.22
4	62.59	66.81	56.74	64.42	63.55	59.15
6	77.76	76.72	69.12	77.67	75.27	73.25
8	99.53	94.44	93.18	86.25	84.68	83.79
12	99.42	97.62	99.27	94.36	99.11	100.21

FT-IR: Using a Bruker alpha spectrophotometer, the FT-IR spectrum of the purchased sesamol sample was acquired. The spectrum was then examined for the distinctive peaks of the functional groups that are present in the compound. Sesamol's infrared spectra showed strong vibrations of the hydroxyl group stretching (3732 cm^-1), C-H (3112 cm^-1), aromatic C-C (1651 cm^-1), and C-O bending (701 cm^-1).

Fig. 2. FT-IR spectrum of sesamol

Fig. 3. FT-IR spectrums of physical mixture of sodium alginate, chitosan and sesamol

Scanning Electron Microscope: The non-porous nature and fibres-free texture of the pure chitosan film are evident. The chitosan film exhibits an aggregation. The structure of the reinforced composite is branch-like. Porosity also rises when cellulose fibre and chitosan are added. The cellulose fibre thickens as the inner layers' fibres become more apparent.

Fig. 4. SEM Analysis of Sesamol Microspheres

Fig. 5. Cumulative drug release graph of Sesamol loaded microspheres

Fig. 6. Yield and particles size of various batches of microspheres

CONCLUSION:

Floating sesamol microspheres were created for the current study. The sample was identified as pure sesamol based on the results of the drug identification tests, which included FTIR and UV visible spectrophotometric analyses. The compatibility of the medicine and excipients was determined by FTIR analysis, which showed no interaction. Sesamol maximum absorbance was measured at 295 nm. Using sodium alginate and chitosan as natural polymers and 5% calcium chloride as the crosslinking counter ion, ionic gelation was used in this study to create microspheres loaded with sesamol. The outcomes demonstrated the methodology's capacity to create repeatable microspheres and provide medication release from formulations over an extended period of time. The formulation F4, which had 1.25 times more chitosan than alginate, was the best formulation with low particle size, high drug content, and drug release for up to 12 hours, according to the overall results for drug content, particle size, and micromeritic characteristics.

ACKNOWLEDGMENT:

I am thankful to Dr. Gagan Kukloria, Dr. Sujit Pillai Principal of GRY Institute of Pharmacy for their guidance and support.

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Received on 31.05.2025 Revised on 21.06.2025

Accepted on 07.07.2025 Published on 25.07.2025

Available online from July 31, 2025

Res. J. Pharma. Dosage Forms and Tech.2025; 17(3):179-182.

DOI: 10.52711/0975-4377.2025.00025

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