Original Article
DESIGN, OPTIMIZATION AND EVALUATION OF RANOLAZINE FAST-DISSOLVING FILMS
EMPLOYING MANGO KERNEL STARCH AS A NEW NATURAL SUPERDISINTEGRANT
MEDISETTY GAYATRI DEVI, SANTOSH KUMAR R.
*
Department of Pharmaceutics, GITAM School of Pharmacy, Visakhapatnam, Andhra Pradesh-530045, India
*
Corresponding author: Santosh Kumar R.;
*
Email: srada@gitam.edu
Received: 19 May 2024, Revised and Accepted: 17 Sep 2024
ABSTRACT
Objective: The BCS class II cardiovascular medication, Ranolazine (RZN), is characterized by limited solubility and inadequate oral absorption. The
objective of the current research is to develop a natural superdisintegrant in the formulation of Fast-Dissolving Films (FDFs) of Cardio Vascular
Drug (CVD) RZN to enhance its dissolution rate, solubility, absorption, and therapeutic action.
Methods: Mango Kernel Starch (MKS) is isolated by grinding the kernels, forming a slurry with water, filtering, and using repeated centrifugation
and washing to purify the starch, which is then dried. The obtained starch is collected. Along with obtained natural superdisintegrant MKS,
Maltodextrin (MDX) and Sodium Starch Glycolate (SSG) were also utilized in the fabrication of FDFs containing RZN via the solvent casting
technique. A total of eight formulations (RF1 to RF8) were developed employing a 2
3
factorial design, using the natural superdisintegrant alone at a
concentration of 5% and in combination with other superdisintegrants.
Results: The prepared MKS was found to be free-flowing, fine, amorphous, insoluble in organic solvents, and exhibiting 0.17% solubility in water
with a swelling index of 89.95%, indicating superdisintegrant properties. Fourier-transform infrared spectroscopy (FTIR) studies and Differential
scanning calorimetry (DSC) analysis indicated that there was no drug-excipient interaction. The films prepared with a 5% concentration of the MKS
showed good physical properties and resulted in an increased drug dissolution rate, with 99.78 % of the drug dissolved within 10 min, along with
the lowest disintegration time of 13.45 sec.
Conclusion: The research successfully isolated a new superdisintegrant, MKS and formulated FDFs of the poorly water-soluble drug RZN. The MKS
was found to be an effective superdisintegrant with no drug interactions, producing films with good physical and mechanical properties, increasing
the drug dissolution rate, and providing rapid disintegration with improved relative bioavailability.
Keywords: Fast dissolving films, FDFs, Ranolazine, Solvent casting technique, Super disintegrant, Mango kernel starch
© 2024 The Authors. Published by Innovare Academic Sciences Pvt Ltd. This is an open access article under the CC BY license (https://creativecommons.org/licenses/by/4.0/)
DOI: https://dx.doi.org/10.22159/ijap.2024v16i6.51506 Journal homepage: https://innovareacademics.in/journals/index.php/ijap
INTRODUCTION
The oral route is the most often used since it is the easiest to administer
and results in high patient compliance. Oral solid dose forms account for
over 60% of all dosage forms; tablets and capsules are the most often
used types [1]. However, there are several limitations for geriatric,
paediatric, or dysphagia patients, people with difficulty swallowing, and
even in animals [2]. As an alternative method to overcome these
limitations, orally disintegrating systems were developed, aiming for a
fast release of the drug without water ingestion, also enabling drug
absorption directly through oral mucosa to enter systemic circulation,
avoiding first-pass hepatic metabolism [3].
Fast-dissolving films (FDFs) are one such novel approach to increase
consumer acceptance by rapid dissolution and self-administration
without water or chewing. The need for non-invasive delivery
systems continues due to patients’ poor acceptance and compliance
with existing delivery regimes, the limited market size for drug
companies and drug uses, coupled with high cost of disease
management [4]. Usually, the casting technique is used to prepare
FDFs with natural polymers, and other techniques like hot-melt
extrusion [5] are frequently used to process synthetic polymers.
FDFs can also be prepared by utilizing other techniques such as
electrospinning [6], freeze-drying [7], and heat-drying methods [8],
which may affect certain characteristics, particularly film thickness.
The choice of the optimal usage of superdisintegrants remains difficult
since they must be able to dissolve in the oral cavity as quickly as
feasible and cost-effectively. Much research has been carried out on
natural superdisintegrants like Starch derivatives (Corn and potato
starch), Alginates, Guar gum, Chitosan and Plantago ovata [9].
Existing research focuses on the efficacy of natural starch as a
superdisintegrant and positions Mango Kernel Starch (MKS) as a
superior alternative [10]. MKS is increasingly utilized as a
superdisintegrant in the optimization and design of FDFs due to its
exceptional disintegration efficiency, biocompatibility, and cost-
effectiveness. Its ability to rapidly absorb water and swell ensures
quick breakdown upon contact with saliva, a critical feature for
FDFs. As a natural, non-toxic material, MKS reduces the risk of
adverse reactions, making it suitable for pharmaceutical
applications. Additionally, its use promotes sustainability by
valorizing a by-product of mango processing, aligning with eco-
friendly manufacturing practices. Accordingly, we examined the
literature in this work to optimize and design FDFs of Ranolazine
(RZN) using MKS as a natural superdisintegrant [11].
The novelty of this research lies in the introduction of MKS as a
novel superdisintegrant in the formulation of FDFs for the
antihypertensive drug RZN. Addressing the challenge of poor water
solubility and limited bioavailability, this study explores the
potential of MKS to enhance the disintegration time and drug
dissolution rate. Traditional superdisintegrants such as Maltodextrin
(MDX) and Sodium Starch Glycolate (SSG) have been widely used,
but the integration of MKS presents a promising alternative due to
its natural origin and superior performance [12].
Statistical analysis using 2
3
factorial design is a method employed for
optimizing the formulation of superdisintegrants in the
manufacturing of films [13]. This approach allows researchers to
systematically evaluate the three critical factors, each at two levels.
This study aims to enhance the dissolution rate with rapid
disintegration and increased relative bioavailability. Such precision
in formulation has the potential to improve therapeutic efficacy and
patient compliance, contributing significantly to advancements in
pharmaceutical research [14].
MATERIALS AND METHODS
Materials RZN, the active pharmaceutical ingredient (API), was a gift
sample obtained from Hyderabad-based Hetero Pvt Ltd. HPMC E15
International Journal of Applied Pharmaceutics
ISSN- 0975-7058 Vol 16, Issue 6, 2024